Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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ligand		 Fold
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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
155524115 350512 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 350512 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 350512 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
46235428 20934 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 20934 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227401 350418 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 350418 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
51354300 121673 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688946 121673 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155491015 350461 6 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 350461 6 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155513612 350289 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 350418 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
45257132 7480 22 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 7480 22 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 7480 22 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155552061 350445 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
155517880 350627 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45257132 7480 22 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 7480 22 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 7480 22 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
58227373 350473 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136030655 119281 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136030655 119281 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25068753 371642 21 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 371642 21 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
10105117 213914 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 213914 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
127051301 277488 0 None 4 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None 4 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
136141537 119280 6 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
4024 4117 17 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 4117 17 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 4117 17 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
58227259 235997 0 None None None Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 235997 0 None None None Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1194 95 1 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 95 1 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 95 1 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
24797598 124320 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1771001 124320 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
11846299 276546 0 None None None Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
CHEMBL378788 276546 0 None None None Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
46228114 445812 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596551 445812 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25130576 370860 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 370860 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130232 370798 0 None None None Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494576 370798 0 None None None Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
25131229 370829 0 None None None Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL494724 370829 0 None None None Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130576 370860 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 370860 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
11846635 160196 0 None None None Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
CHEMBL211242 160196 0 None None None Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
46228132 465650 0 None None None Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL609161 465650 0 None None None Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
25129178 370863 0 None None None Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494910 370863 0 None None None Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
1267 8287 36 None -10 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
3035905 8287 36 None -10 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
CHEMBL260374 8287 36 None -10 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
44480708 20107 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
CHEMBL1078632 20107 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
53233804 124284 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770966 124284 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
1247 7944 80 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 7944 80 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 7944 80 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 7944 80 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
127052293 277526 5 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
45257131 444119 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 444119 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
56593499 277530 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3805392 277530 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
127050776 277535 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805437 277535 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
127050431 277603 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 277603 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227165 235977 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393536 235977 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
25130578 370576 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493099 370576 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
25129525 370817 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494648 370817 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
25128833 371611 26 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 371611 26 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25128831 337127 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 337127 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
11043445 116511 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL1632410 116511 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
16061839 371625 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL502104 371625 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
127050431 277603 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 277603 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
54585780 124316 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770998 124316 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
1247 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
25130914 370502 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL492677 370502 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
11957573 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
1250 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
3692 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
CHEMBL19439 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
11957573 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 4107 26 None -54 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1253 4209 4 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 4209 4 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 4209 4 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10176414 8813 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 8813 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 8813 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1267 8287 36 None -10 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -10 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -10 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
44482032 20065 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078346 20065 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25130581 370474 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 370474 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
44482029 19967 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
CHEMBL1077737 19967 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
25131234 370896 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495083 370896 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
25130235 370821 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 370821 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 370821 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 370821 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
25130234 370641 0 None None None Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493663 370641 0 None None None Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
127051986 277592 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806098 277592 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
51354301 121676 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
CHEMBL1688969 121676 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
10934158 212958 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 212958 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10017821 213508 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 213508 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
1238 4258 10 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 4258 10 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 4258 10 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11043445 116511 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 116511 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10945113 212986 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 212986 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
44480707 20095 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078529 20095 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
10945113 212986 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL322256 212986 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
127052294 277590 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 277590 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 7944 80 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
10934158 212958 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 212958 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
25129182 370530 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492869 370530 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
127052293 277526 5 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11846634 159587 0 None None None Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209758 159587 0 None None None Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
11846464 160015 0 None None None Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
CHEMBL211170 160015 0 None None None Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
25071319 372221 16 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 372221 16 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44482030 20005 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
CHEMBL1077860 20005 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
25131561 370642 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 370642 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
135897837 370862 11 None None None Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494909 370862 11 None None None Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
127048828 277608 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806255 277608 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227255 235980 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393539 235980 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
44568832 370432 0 None None None Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492242 370432 0 None None None Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
25128822 370716 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 370716 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
1251 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
3035842 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
CHEMBL18661 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
1251 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 4115 26 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
25149712 352886 0 None -6 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL470790 352886 0 None -6 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
25149335 365842 0 None -6 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL483406 365842 0 None -6 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1279 7960 58 None 2 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 7960 58 None 2 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 7960 58 None 2 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
127048890 277583 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805995 277583 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
46890548 20914 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083084 20914 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44481761 20106 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
CHEMBL1078631 20106 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
51354301 121676 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 121676 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155513612 350289 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1248 2933 20 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 2933 20 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 2933 20 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 2933 20 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
5310982 194029 1 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 194029 1 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
1269 249 35 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 249 35 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 249 35 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
53233802 124305 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770987 124305 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
25131559 370819 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 370819 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
1247 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
44480959 20006 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077861 20006 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
1484519 347971 43 None None None Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL454007 347971 43 None None None Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
21638785 371849 3 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 371849 3 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127051958 277566 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805813 277566 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25129880 385668 0 None None None Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522841 385668 0 None None None Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
25130231 370937 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495280 370937 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
25131228 370828 0 None None None Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494723 370828 0 None None None Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128828 371469 0 None None None Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL499631 371469 0 None None None Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
58227163 350430 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25071319 372221 16 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 372221 16 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1247 7944 80 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 7944 80 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 7944 80 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 7944 80 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
25130233 335164 6 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL445091 335164 6 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
25128831 337127 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 337127 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
25130574 370615 0 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
CHEMBL493461 370615 0 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
44568790 335952 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL446269 335952 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
155552061 350445 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
45257133 444104 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 444104 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
11846300 161722 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
1247 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3032915 39388 20 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 39388 20 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
53321919 119278 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 119278 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10060213 202962 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 202962 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
25128823 385260 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 385260 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
25131230 385649 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522679 385649 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
10037650 19547 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 19547 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
170389 473913 24 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 473913 24 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155513612 350289 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136141537 119280 6 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136192874 119282 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
46228133 444980 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595639 444980 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10197870 19637 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106612 19637 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10197870 19637 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106612 19637 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10879463 19627 0 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106570 19627 0 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1279 7960 58 None -2 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 7960 58 None -2 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 7960 58 None -2 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 7960 58 None -2 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 7960 58 None -2 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 7960 58 None -2 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
58227260 235987 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393546 235987 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
11846636 159535 0 None None None Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209628 159535 0 None None None Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
1247 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
16061961 432771 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 432771 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1247 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1375 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
774 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
CHEMBL90 7944 80 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
127052635 277495 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805003 277495 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25130237 370529 0 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492864 370529 0 None None None Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
127051301 277488 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25131555 370428 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492227 370428 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
25130914 370502 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL492677 370502 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10879463 19627 0 None None None Human 4.7 pEC50 = 4.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106570 19627 0 None None None Human 4.7 pEC50 = 4.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
1613 4786 46 None None None Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 4786 46 None None None Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 4786 46 None None None Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 4786 46 None None None Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 4786 46 None None None Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
753256 353242 8 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL473662 353242 8 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
25131560 370588 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493229 370588 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
1223 1963 35 None -13 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
2790 1963 35 None -13 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
CHEMBL14690 1963 35 None -13 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
155512725 350210 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
10037650 19547 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 19547 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
25129881 370431 5 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492241 370431 5 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
44568855 385723 0 None None None Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
CHEMBL523335 385723 0 None None None Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
25128832 336539 0 None None None Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
CHEMBL447151 336539 0 None None None Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
25071940 370596 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 370596 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
127049156 277482 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3804837 277482 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
11437850 370895 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495082 370895 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
25129883 385266 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522019 385266 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25133972 370592 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
CHEMBL493262 370592 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
25130575 370823 2 None None None Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494687 370823 2 None None None Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130577 337112 0 None None None Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL449021 337112 0 None None None Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
10773349 22407 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 22407 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
127052634 277597 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3806146 277597 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
90667240 219049 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL3220642 219049 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
25130576 370860 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 370860 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25128826 371996 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL506187 371996 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130576 370860 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 370860 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
58227157 234852 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354815 234852 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
1247 7944 80 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 7944 80 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 7944 80 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 7944 80 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1226 4125 18 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 4125 18 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 4125 18 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
25133970 370822 1 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL494679 370822 1 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130230 336976 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 336976 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
1269 249 35 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 249 35 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 249 35 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
44480958 20003 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
CHEMBL1077859 20003 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
25131556 372047 6 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 372047 6 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
127051047 277599 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806162 277599 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
45257134 444353 0 None None None Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
CHEMBL594949 444353 0 None None None Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
25131231 370436 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492288 370436 0 None None None Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
10381810 470034 0 None None None Human 7.6 pEC50 = 7.6 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL7828 470034 0 None None None Human 7.6 pEC50 = 7.6 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
155512725 350210 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
127052294 277590 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 277590 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25128822 370716 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 370716 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
155491015 350461 6 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 350461 6 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
46890072 21239 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084355 21239 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 21636 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 21636 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227373 350473 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
21638785 371849 3 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 371849 3 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
25130911 368528 0 None None None Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL485802 368528 0 None None None Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
16352 236038 7 None None None Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 236038 7 None None None Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
1267 8287 36 None -8 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -8 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -8 4 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
25130579 370944 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL495341 370944 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
10678661 19698 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 19698 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
46228101 443435 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594022 443435 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1249 4105 12 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 4105 12 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 4105 12 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1269 249 35 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 249 35 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 249 35 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
25129528 370435 0 None None None Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492287 370435 0 None None None Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
44568923 385643 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522661 385643 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
67087450 235991 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393550 235991 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
44547127 234853 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354816 234853 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227148 235988 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 235988 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
10678661 19698 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 19698 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
25131557 385785 0 None None None Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
CHEMBL523835 385785 0 None None None Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
25130909 370619 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 370619 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
44478385 20108 8 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 20108 8 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
46890549 20915 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083085 20915 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44480960 19961 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077636 19961 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
42625303 354634 0 None -2089 7 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
CHEMBL475621 354634 0 None -2089 7 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
56954425 163508 0 None -16 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165643 163508 0 None -16 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
25130913 334745 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444484 334745 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
1274 8815 10 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 8815 10 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 8815 10 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
155517880 350627 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 350445 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
25129180 370499 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL492662 370499 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
3228743 370620 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493479 370620 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
12769844 219048 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
CHEMBL3220641 219048 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
25129181 370500 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492663 370500 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
25128825 370799 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494585 370799 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
44478385 20108 8 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
CHEMBL1078642 20108 8 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
44478385 20108 8 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL1078642 20108 8 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
25129527 370651 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493720 370651 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
24798596 443897 0 None None None Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594491 443897 0 None None None Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127052292 277554 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805663 277554 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1274 8815 10 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 8815 10 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 8815 10 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
11846465 279116 0 None None None Human 7.4 pEC50 = 7.4 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
CHEMBL387054 279116 0 None None None Human 7.4 pEC50 = 7.4 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
25131559 370819 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 370819 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
25131561 370642 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 370642 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
46235428 20934 0 None -263 3 Mouse 7.4 pEC50 = 7.4 Functional
Intrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 20934 0 None -263 3 Mouse 7.4 pEC50 = 7.4 Functional
Intrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1269 249 35 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 249 35 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 249 35 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
136030655 119281 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25129523 370534 40 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492884 370534 40 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129523 370534 40 None None None Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 370534 40 None None None Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
70692530 157356 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL2047474 157356 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
91613 41853 21 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 41853 21 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
58227326 235983 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393542 235983 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
58227373 350473 0 None -3 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None -3 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
25071004 385261 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 385261 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
42625303 354634 0 None -2 7 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
CHEMBL475621 354634 0 None -2 7 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
25128824 385707 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 385707 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
10702196 212956 1 None -1 2 Human 4.4 pEC50 = 4.4 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL320279 212956 1 None -1 2 Human 4.4 pEC50 = 4.4 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
56954320 163506 0 None -12 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165641 163506 0 None -12 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
1267 8287 36 None -10 4 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
3035905 8287 36 None -10 4 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
CHEMBL260374 8287 36 None -10 4 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
25129524 370433 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL492274 370433 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130909 370619 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 370619 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
1279 7960 58 None -2 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 7960 58 None -2 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 7960 58 None -2 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
25128833 371611 26 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 371611 26 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25129526 370650 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493719 370650 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
24797248 443894 0 None None None Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594490 443894 0 None None None Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127050434 277538 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
CHEMBL3805514 277538 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
25129169 370430 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 370430 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
24798595 334930 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444782 334930 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
90667239 219047 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
CHEMBL3220640 219047 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
25130573 370144 1 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL489663 370144 1 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130581 370474 0 None -3 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 370474 0 None -3 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25130235 370821 1 None -4 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 370821 1 None -4 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
46890546 20845 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082771 20845 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46228143 445184 0 None None None Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595880 445184 0 None None None Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
117724523 235970 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393529 235970 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
25130914 370502 0 None -15 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 370502 0 None -15 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129179 370901 1 None None None Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL495112 370901 1 None None None Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25130236 370934 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 370934 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
25068753 371642 21 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 371642 21 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
53233805 124282 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770964 124282 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
46890545 21705 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086460 21705 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1274 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
1274 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
3063228 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
CHEMBL1196470 8815 10 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
136141537 119280 6 None -5 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None -5 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
11313837 5081 11 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 5081 11 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 5081 11 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
10583206 212980 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321920 212980 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
155513612 350289 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155512725 350210 0 None -6 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None -6 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
58227163 350430 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25130580 348358 0 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL455016 348358 0 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25129878 370578 0 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493103 370578 0 None None None Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
127052295 277485 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 352 7 3 4 2.4 N#C/N=C(/NCCOc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804862 277485 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 352 7 3 4 2.4 N#C/N=C(/NCCOc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
53233803 124280 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770962 124280 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
25129169 370430 0 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 370430 0 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
127049856 277533 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805431 277533 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
90667238 219046 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
CHEMBL3220639 219046 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
565544 212992 10 None -4466 2 Human 6.3 pEC50 = 6.3 Functional
Inhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
CHEMBL322988 212992 10 None -4466 2 Human 6.3 pEC50 = 6.3 Functional
Inhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
10583206 212980 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321920 212980 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
25130915 370535 1 None None None Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL492885 370535 1 None None None Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
46228125 444588 0 None None None Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595215 444588 0 None None None Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
44482028 19955 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccn1 10.1021/jm900526h
CHEMBL1077580 19955 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccn1 10.1021/jm900526h
25131232 370537 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL492900 370537 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130235 370821 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 370821 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 370821 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 370821 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
45257133 444104 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 444104 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25128824 385707 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 385707 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
155517880 350627 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45269820 390145 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL551790 390145 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
25071004 385261 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 385261 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
46890022 21374 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084869 21374 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46228158 465674 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL609289 465674 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890547 20846 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
CHEMBL1082772 20846 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
1255 6493 23 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 6493 23 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 6493 23 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
9974306 469376 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 469376 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
10060212 469434 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72769 469434 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
136192874 119282 0 None 1 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None 1 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1237 7956 17 None -380 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 7956 17 None -380 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 7956 17 None -380 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
25129175 370618 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493477 370618 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130914 370502 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 370502 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25130908 336381 1 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL446896 336381 1 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
24797775 370493 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492631 370493 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
1247 7944 80 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25130912 371925 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505061 371925 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
1247 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25149521 352953 0 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL471413 352953 0 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1375 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
774 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
CHEMBL90 7944 80 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1267 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
1269 249 35 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
37463 249 35 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
CHEMBL275443 249 35 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
1267 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 8287 36 None -10 4 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
44482031 19973 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077756 19973 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
46890019 21632 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086085 21632 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
156015638 352187 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -2 4 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
4908365 7960 58 None -2 4 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
CHEMBL129198 7960 58 None -2 4 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
10978141 19489 0 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL105803 19489 0 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
58227127 235984 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393543 235984 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
44481489 20046 0 None 18 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078210 20046 0 None 18 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
10419556 19694 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106913 19694 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
11086114 21714 0 None None None Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL108649 21714 0 None None None Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
10820930 20131 0 None None None Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL107877 20131 0 None None None Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
10106063 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321860 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10106063 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
CHEMBL321860 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
56954318 163505 0 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165640 163505 0 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
10106063 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321860 212979 11 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10017000 469387 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL72431 469387 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
136192874 119282 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1267 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
3035905 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
CHEMBL260374 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
1240 4168 15 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 4168 15 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 4168 15 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10978141 19489 0 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 19489 0 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
1279 7960 58 None -2 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
4908365 7960 58 None -2 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
CHEMBL129198 7960 58 None -2 4 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
42625303 354634 0 None -501 7 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
CHEMBL475621 354634 0 None -501 7 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
10419556 19694 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106913 19694 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11086114 21714 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL108649 21714 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
155513612 350289 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
25130230 336976 0 None -3 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 336976 0 None -3 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
25133971 370591 1 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL493261 370591 1 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130229 371938 4 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505346 371938 4 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
56954515 163492 0 None -16 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 163492 0 None -16 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
56954322 163507 0 None -10 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 163507 0 None -10 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
45257131 444119 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 444119 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
11846298 276604 0 None None None Human 7.1 pEC50 = 7.1 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
CHEMBL379102 276604 0 None None None Human 7.1 pEC50 = 7.1 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
25129176 346890 0 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
CHEMBL451108 346890 0 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
58227388 235979 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393538 235979 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
1223 1963 35 None -501 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
2790 1963 35 None -501 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
CHEMBL14690 1963 35 None -501 3 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
10820929 212948 1 None -30 2 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL319658 212948 1 None -30 2 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
53233801 124303 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770985 124303 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
58227252 235985 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393544 235985 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
1247 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1274 8815 10 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 8815 10 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 8815 10 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
25130236 370934 0 None -1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 370934 0 None -1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
1267 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 8287 36 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
25129877 334036 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL442865 334036 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
44568847 370497 0 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492652 370497 0 None None None Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25101945 385646 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 385646 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
25101945 385646 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 385646 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
58227143 235982 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393541 235982 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
16061961 432771 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 432771 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
112936251 274671 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 274671 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
58227163 350430 0 None -8 3 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None -8 3 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25131556 372047 6 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 372047 6 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128830 370945 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
CHEMBL495342 370945 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
127035835 274690 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 274690 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
11983344 20007 2 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077862 20007 2 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25128829 370577 0 None None None Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493100 370577 0 None None None Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
24745335 607 14 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 607 14 None None None Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None None None Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None None None Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None None None Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
156013896 352155 0 None 16 2 Human 8.8 pIC50 = 8.8 Functional
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None 16 2 Human 8.8 pIC50 = 8.8 Functional
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
44129134 431638 0 None None None Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 431638 0 None None None Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
56835171 141988 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 141988 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
16082828 155180 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213886 155180 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
71525678 180554 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 180554 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
71525679 180555 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 180555 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
1279 7960 58 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
4908365 7960 58 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
CHEMBL129198 7960 58 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
10446295 4352 37 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 4352 37 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 4352 37 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
155563181 349313 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 498 12 1 7 5.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccc(OCCCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.9b00937
CHEMBL4573309 349313 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 498 12 1 7 5.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccc(OCCCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.9b00937
25147771 348296 0 None None None Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 348296 0 None None None Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
16082833 161802 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214312 161802 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
90645145 221665 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290578 221665 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
1267 8287 36 None -4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
3035905 8287 36 None -4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
CHEMBL260374 8287 36 None -4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
1279 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
4908365 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
CHEMBL129198 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
3201696 39659 3 None -22 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222728 39659 3 None -22 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
1279 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
63868328 348309 1 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4549015 348309 1 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71548412 3905 26 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 3905 26 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 3905 26 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
16656871 22292 0 None None None Human 6.5 pIC50 = 6.5 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090531 22292 0 None None None Human 6.5 pIC50 = 6.5 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
16718567 22478 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091874 22478 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1279 7960 58 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
155540438 337059 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4483783 337059 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
44129130 432014 0 None None None Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 432014 0 None None None Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11682208 22590 0 None None None Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1092542 22590 0 None None None Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
25112105 22479 0 None None None Human 8.4 pIC50 = 8.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091875 22479 0 None None None Human 8.4 pIC50 = 8.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
24745335 607 14 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
1279 7960 58 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 7960 58 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 7960 58 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
16656872 22229 0 None None None Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090190 22229 0 None None None Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
122193095 251968 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628042 251968 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
49841846 141986 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 141986 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
49841719 141985 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 141985 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
1279 7960 58 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
90645147 221663 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290576 221663 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
24745335 607 14 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 607 14 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 607 14 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 607 14 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
10446295 4352 37 None None None Human 6.3 pIC50 = 6.3 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 4352 37 None None None Human 6.3 pIC50 = 6.3 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 4352 37 None None None Human 6.3 pIC50 = 6.3 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
122194625 252070 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
CHEMBL3629828 252070 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
1267 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
3035905 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
CHEMBL260374 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
1267 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3035905 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
CHEMBL260374 8287 36 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
25147772 347506 9 None None None Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 347506 9 None None None Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
71548412 3905 26 None -12 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 3905 26 None -12 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 3905 26 None -12 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
11709443 22562 0 None None None Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092332 22562 0 None None None Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71519674 180558 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 180558 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
16656874 22422 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091569 22422 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
49841845 141987 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 141987 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
156013896 352155 0 None -16 2 Mouse 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -16 2 Mouse 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 7960 58 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 7960 58 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
16082831 155181 0 None -100 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL214311 155181 0 None -100 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
71525681 180557 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 180557 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
1267 8287 36 None -4 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 8287 36 None -4 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 8287 36 None -4 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
58227148 235988 0 None None None Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 235988 0 None None None Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
59777258 219673 0 None None None Human 10.0 pKd = 10 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236561 219673 0 None None None Human 10.0 pKd = 10 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
24797604 219664 0 None None None Human 9.9 pKd = 9.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
CHEMBL3236552 219664 0 None None None Human 9.9 pKd = 9.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
24994542 219666 0 None None None Human 9.6 pKd = 9.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236554 219666 0 None None None Human 9.6 pKd = 9.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
24798144 219665 0 None None None Human 9.5 pKd = 9.5 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 219665 0 None None None Human 9.5 pKd = 9.5 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
53257796 219687 0 None None None Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236575 219687 0 None None None Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
54587790 124298 0 None None None Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770980 124298 0 None None None Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
24745337 124297 0 None None None Human 9.3 pKd = 9.3 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770979 124297 0 None None None Human 9.3 pKd = 9.3 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
59777338 219668 0 None None None Human 9.2 pKd = 9.2 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236556 219668 0 None None None Human 9.2 pKd = 9.2 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
44547268 235967 0 None None None Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393526 235967 0 None None None Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227340 235973 0 None None None Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393532 235973 0 None None None Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
58227200 235976 0 None None None Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393535 235976 0 None None None Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
54585781 124319 0 None None None Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1771000 124319 0 None None None Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
54583873 124287 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770969 124287 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
54587787 124289 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770971 124289 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
54581940 124310 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770992 124310 0 None None None Human 8.8 pKd = 8.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
25130912 371925 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL505061 371925 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
23653543 140320 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914541 140320 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
24994636 219677 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
CHEMBL3236565 219677 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
42624149 219680 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 219680 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
59777262 219684 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236572 219684 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
54584824 124295 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770977 124295 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227337 235994 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393553 235994 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
58227259 235997 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 235997 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
24798144 219665 0 None None None Mouse 8.0 pKd = 8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 219665 0 None None None Mouse 8.0 pKd = 8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
24826766 135881 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914750 135881 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
9944571 235882 0 None None None Human 8.0 pKd = 8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338937 235882 0 None None None Human 8.0 pKd = 8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
24994634 4374 36 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
53258370 219681 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236569 219681 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
24994635 219682 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236570 219682 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
54582865 124277 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770959 124277 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
54584825 124308 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770990 124308 0 None None None Human 7.9 pKd = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
11587279 253067 3 None None None Human 7.9 pKd = 7.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
CHEMBL364400 253067 3 None None None Human 7.9 pKd = 7.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
46890627 20919 0 None None None Human 7.9 pKd = 7.9 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083098 20919 0 None None None Human 7.9 pKd = 7.9 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
66740470 219355 0 None None None Human 6.9 pKd = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3233048 219355 0 None None None Human 6.9 pKd = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
11687917 38863 0 None None None Human 6.9 pKd = 6.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
CHEMBL120854 38863 0 None None None Human 6.9 pKd = 6.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
9966927 42734 3 None None None Human 6.9 pKd = 6.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL128252 42734 3 None None None Human 6.9 pKd = 6.9 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
54581938 124290 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770972 124290 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
67087450 235991 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393550 235991 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
11594278 38594 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL120591 38594 0 None None None Human 7.8 pKd = 7.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
9923162 42797 10 None None None Human 7.8 pKd = 7.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128613 42797 10 None None None Human 7.8 pKd = 7.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
11120826 42777 2 None None None Human 6.8 pKd = 6.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128505 42777 2 None None None Human 6.8 pKd = 6.8 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
46890677 21611 0 None None None Human 6.8 pKd = 6.8 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086038 21611 0 None None None Human 6.8 pKd = 6.8 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 21636 0 None None None Mouse 4.8 pKd = 4.8 Functional
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 21636 0 None None None Mouse 4.8 pKd = 4.8 Functional
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
66740898 219674 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
CHEMBL3236562 219674 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
10468601 390593 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activityAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activity
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL555434 390593 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activityAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activity
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
53233904 124283 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770965 124283 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
10446295 4352 37 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 4352 37 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 4352 37 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
4242975 42701 7 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128088 42701 7 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
9900313 43276 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129444 43276 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
9839217 144732 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199062 144732 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
11565330 197533 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
CHEMBL268525 197533 0 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
4906599 333322 9 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL436381 333322 9 None None None Human 7.7 pKd = 7.7 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
24996854 219676 0 None None None Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
CHEMBL3236564 219676 0 None None None Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
42624150 219689 0 None None None Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236577 219689 0 None None None Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
24797956 219670 1 None None None Human 7.6 pKd = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 219670 1 None None None Human 7.6 pKd = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
24992735 219695 0 None None None Human 7.6 pKd = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
CHEMBL3236582 219695 0 None None None Human 7.6 pKd = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
10244243 278547 0 None None None Human 7.6 pKd = 7.6 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL383384 278547 0 None None None Human 7.6 pKd = 7.6 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
46890592 20722 0 None None None Human 7.6 pKd = 7.6 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 20722 0 None None None Human 7.6 pKd = 7.6 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44547127 234853 0 None None None Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354816 234853 0 None None None Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
24992077 219683 0 None None None Human 8.4 pKd = 8.4 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236571 219683 0 None None None Human 8.4 pKd = 8.4 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
10934567 43114 0 None None None Human 7.5 pKd = 7.5 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL129026 43114 0 None None None Human 7.5 pKd = 7.5 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
11630326 144784 0 None None None Human 7.5 pKd = 7.5 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199231 144784 0 None None None Human 7.5 pKd = 7.5 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
44547567 235974 0 None None None Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393533 235974 0 None None None Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
4060730 43234 34 None None None Human 7.4 pKd = 7.4 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129199 43234 34 None None None Human 7.4 pKd = 7.4 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
53378711 219690 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236578 219690 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
24994634 4374 36 None None None Mouse 8.3 pKd = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None None None Mouse 8.3 pKd = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None None None Mouse 8.3 pKd = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
54753437 140454 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915048 140454 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
42624149 219680 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 219680 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
46890590 21353 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084810 21353 0 None None None Mouse 7.3 pKd = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
11572877 139367 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL187285 139367 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
9992865 233442 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL333220 233442 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
11601630 260678 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL370135 260678 0 None None None Human 7.3 pKd = 7.3 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
46890546 20845 0 None None None Human 7.3 pKd = 7.3 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082771 20845 0 None None None Human 7.3 pKd = 7.3 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890590 21353 0 None None None Human 7.3 pKd = 7.3 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084810 21353 0 None None None Human 7.3 pKd = 7.3 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
2063135 22692 6 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1093180 22692 6 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
11066922 43275 0 None None None Human 8.2 pKd = 8.2 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129436 43275 0 None None None Human 8.2 pKd = 8.2 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
24994634 4374 36 None None None Rat 7.2 pKd = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None None None Rat 7.2 pKd = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None None None Rat 7.2 pKd = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
10083188 278200 2 None None None Human 7.2 pKd = 7.2 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL382276 278200 2 None None None Human 7.2 pKd = 7.2 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
46890019 21632 0 None None None Human 7.2 pKd = 7.2 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086085 21632 0 None None None Human 7.2 pKd = 7.2 Functional
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1279 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
10967174 43294 1 None None None Human 8.1 pKd = 8.1 Functional
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 43294 1 None None None Human 8.1 pKd = 8.1 Functional
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
42624148 219686 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236574 219686 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
54583875 124313 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770995 124313 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227179 235989 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393548 235989 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
58227086 235998 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393557 235998 0 None None None Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1279 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 7960 58 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
10967174 43294 1 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129540 43294 1 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
10988959 236934 2 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL340740 236934 2 None None None Human 8.1 pKd = 8.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
10923241 43019 1 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128958 43019 1 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
9878733 235727 1 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338051 235727 1 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
11623296 235888 0 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338972 235888 0 None None None Human 7.1 pKd = 7.1 Functional
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
16202258 140489 0 None None None Human 10.5 pKi = 10.5 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915536 140489 0 None None None Human 10.5 pKi = 10.5 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
24745506 140490 0 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915537 140490 0 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
24745335 607 14 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None None None Human 8.8 pKi = 8.8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
44187557 390404 0 None None None Human 8.8 pKi = 8.8 Functional
Agonistic activity at histamine H4 receptorAgonistic activity at histamine H4 receptor
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm1013488
CHEMBL553423 390404 0 None None None Human 8.8 pKi = 8.8 Functional
Agonistic activity at histamine H4 receptorAgonistic activity at histamine H4 receptor
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm1013488
135525668 140483 0 None None None Human 8.0 pKi = 8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915348 140483 0 None None None Human 8.0 pKi = 8 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
136042270 142161 0 None None None Human 7.9 pKi = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938979 142161 0 None None None Human 7.9 pKi = 7.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
24745507 140491 0 None None None Human 7.9 pKi = 7.9 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915538 140491 0 None None None Human 7.9 pKi = 7.9 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
57401167 142115 0 None None None Human 6.9 pKi = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938846 142115 0 None None None Human 6.9 pKi = 6.9 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400778 140481 0 None None None Human 6.8 pKi = 6.8 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915346 140481 0 None None None Human 6.8 pKi = 6.8 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
135525668 140483 0 None None None Human 7.8 pKi = 7.8 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915348 140483 0 None None None Human 7.8 pKi = 7.8 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57391926 142148 0 None None None Human 6.7 pKi = 6.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938967 142148 0 None None None Human 6.7 pKi = 6.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042269 142160 0 None None None Human 7.7 pKi = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938978 142160 0 None None None Human 7.7 pKi = 7.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57402929 142113 0 None None None Human 6.7 pKi = 6.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938844 142113 0 None None None Human 6.7 pKi = 6.7 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57395538 140482 0 None None None Human 6.6 pKi = 6.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915347 140482 0 None None None Human 6.6 pKi = 6.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042267 142158 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938976 142158 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400777 140480 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915345 140480 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
57400777 140480 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915345 140480 0 None None None Human 7.6 pKi = 7.6 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
49841846 141986 0 None None None Human 8.5 pKi = 8.5 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 141986 0 None None None Human 8.5 pKi = 8.5 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
11688307 142149 0 None None None Human 5.5 pKi = 5.5 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938968 142149 0 None None None Human 5.5 pKi = 5.5 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
54754351 140488 0 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915535 140488 0 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
57400778 140481 0 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915346 140481 0 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
10446295 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
1277 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL185951 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
10446295 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
1277 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL185951 4352 37 None None None Human 7.4 pKi = 7.4 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
49841719 141985 0 None None None Human 8.4 pKi = 8.4 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 141985 0 None None None Human 8.4 pKi = 8.4 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
57391927 142150 0 None None None Human 5.4 pKi = 5.4 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938969 142150 0 None None None Human 5.4 pKi = 5.4 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
1279 7960 58 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 7960 58 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 7960 58 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
49841845 141987 0 None None None Human 8.3 pKi = 8.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 141987 0 None None None Human 8.3 pKi = 8.3 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
57395538 140482 0 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915347 140482 0 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
136042265 142156 0 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938974 142156 0 None None None Human 7.3 pKi = 7.3 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57395620 140487 0 None None None Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915534 140487 0 None None None Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
57395620 140487 0 None None None Human 6.2 pKi = 6.2 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915534 140487 0 None None None Human 6.2 pKi = 6.2 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
1279 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
4908365 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL129198 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
1279 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 7960 58 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1267 8287 36 None None None Human 7.2 pKi = 7.2 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 8287 36 None None None Human 7.2 pKi = 7.2 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 8287 36 None None None Human 7.2 pKi = 7.2 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
56835171 141988 0 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 141988 0 None None None Human 8.2 pKi = 8.2 Functional
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
57390145 142152 0 None None None Human 5.1 pKi = 5.1 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938970 142152 0 None None None Human 5.1 pKi = 5.1 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
136042268 142159 0 None None None Human 8.0 pKi = 8.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938977 142159 0 None None None Human 8.0 pKi = 8.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042266 142157 0 None None None Human 8.0 pKi = 8.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938975 142157 0 None None None Human 8.0 pKi = 8.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
54754351 140488 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915535 140488 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
56950378 142114 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938845 142114 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
135 5144 38 None None None Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 5144 38 None None None Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 5144 38 None None None Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 5144 38 None None None Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 5144 38 None None None Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3158 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
667468 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
956 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
CHEMBL101740 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
CHEMBL1628227 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
DB01142 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
DB14750 18465 32 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
2529 347569 76 None 60 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
5344 347569 76 None 60 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 347569 76 None 60 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
DB00263 347569 76 None 60 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
1272 1720 0 None None None Human 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943
O15467 1720 0 None None None Human 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943


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51354301 121676 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
CHEMBL1688969 121676 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
70692530 157356 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL2047474 157356 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
90667434 219059 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220892 219059 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
44367568 99019 3 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153051 99019 3 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
9877454 470443 2 None None None Human 5.0 pEC50 = 5.0 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL81644 470443 2 None None None Human 5.0 pEC50 = 5.0 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
155512725 350210 0 None None None Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None None None Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
1267 8287 36 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
3035905 8287 36 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
CHEMBL260374 8287 36 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
9793791 99292 5 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
CHEMBL153284 99292 5 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
155524115 350512 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1237 7956 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
156615 7956 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
CHEMBL268229 7956 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
46890592 20722 0 None None None Mouse 5.9 pEC50 = 5.9 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 20722 0 None None None Mouse 5.9 pEC50 = 5.9 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 21636 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 21636 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1247 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1279 7960 58 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
4908365 7960 58 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL129198 7960 58 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
155524115 350512 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 350512 0 None None None Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
11344458 470058 0 None None None Human 5.9 pEC50 = 5.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78497 470058 0 None None None Human 5.9 pEC50 = 5.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
1247 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 7944 80 None None None Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
24797956 219670 1 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 219670 1 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
58227373 350473 0 None None None Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None None None Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 350445 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
46887115 22825 0 None None None Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094144 22825 0 None None None Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
58227373 350473 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155517880 350627 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
25149335 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
CHEMBL483406 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
25149335 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL483406 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
25149335 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 365842 0 None None None Human 7.8 pEC50 = 7.8 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
45267230 393431 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL563342 393431 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
42625223 353809 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
CHEMBL474617 353809 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
11240759 214910 1 None None None Human 5.8 pEC50 = 5.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL311473 214910 1 None None None Human 5.8 pEC50 = 5.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
9812843 470101 1 None None None Human 4.8 pEC50 = 4.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78838 470101 1 None None None Human 4.8 pEC50 = 4.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
11469514 213887 0 None None None Human 5.8 pEC50 = 5.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL309654 213887 0 None None None Human 5.8 pEC50 = 5.8 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
155524115 350512 0 None None None Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None None None Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
127052293 277526 5 None None None Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None None None Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
155513612 350289 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42626109 353655 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474447 353655 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
155512725 350210 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
42625386 352268 0 None None None Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 352268 0 None None None Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
46830167 23073 0 None None None Human 8.6 pEC50 = 8.6 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 23073 0 None None None Human 8.6 pEC50 = 8.6 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
11171320 99202 2 None None None Human 5.7 pEC50 = 5.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153207 99202 2 None None None Human 5.7 pEC50 = 5.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1 10.1021/jm030905y
170389 473913 24 None None None Human 6.7 pEC50 = 6.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm030905y
CHEMBL91353 473913 24 None None None Human 6.7 pEC50 = 6.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm030905y
46887041 23072 1 None None None Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 23072 1 None None None Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
155517880 350627 0 None None None Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None None None Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None None None Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
127052293 277526 5 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11301441 196507 12 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL260549 196507 12 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/acs.jmedchem.8b00435
1279 7960 58 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
4908365 7960 58 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
CHEMBL129198 7960 58 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
58227401 350418 0 None None None Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None None None Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None None None Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None None None Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42625222 353657 0 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474449 353657 0 None None None Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
1267 8287 36 None None None Mouse 7.6 pEC50 = 7.6 Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None None None Mouse 7.6 pEC50 = 7.6 Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None None None Mouse 7.6 pEC50 = 7.6 Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
90667228 219039 0 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220629 219039 0 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
58227401 350418 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42625303 354634 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 354634 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
42625304 353001 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 353001 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
11286909 470140 0 None None None Human 5.5 pEC50 = 5.5 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL79126 470140 0 None None None Human 5.5 pEC50 = 5.5 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
9964223 470510 6 None None None Human 4.5 pEC50 = 4.5 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL82244 470510 6 None None None Human 4.5 pEC50 = 4.5 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
42626111 372812 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL515428 372812 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
1247 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
58227373 350473 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 350445 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
58227163 350430 0 None None None Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None None None Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
127050776 277535 0 None None None Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805437 277535 0 None None None Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None None None Rat 5.4 pEC50 = 5.4 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None None None Rat 5.4 pEC50 = 5.4 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None None None Rat 5.4 pEC50 = 5.4 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None None None Rat 5.4 pEC50 = 5.4 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
45269820 390145 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL551790 390145 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
155512725 350210 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
16078981 97364 8 None None None Human 5.4 pEC50 = 5.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1 10.1021/jm030905y
CHEMBL151467 97364 8 None None None Human 5.4 pEC50 = 5.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1 10.1021/jm030905y
155524115 350512 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
46887043 23075 0 None None None Human 8.3 pEC50 = 8.3 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 23075 0 None None None Human 8.3 pEC50 = 8.3 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
42625384 334341 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 334341 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
44367567 327789 2 None None None Human 6.4 pEC50 = 6.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL440730 327789 2 None None None Human 6.4 pEC50 = 6.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
58227163 350430 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 350289 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
156013896 352155 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
127049855 277516 0 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805220 277516 0 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11957573 4107 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
1250 4107 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
3692 4107 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL19439 4107 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
155513612 350289 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None None None Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
127051301 277488 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1247 7944 80 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1375 7944 80 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
774 7944 80 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90 7944 80 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
46235428 20934 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 20934 0 None None None Mouse 6.3 pEC50 = 6.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1251 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
3035842 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
CHEMBL18661 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
1251 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
3035842 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
CHEMBL18661 4115 26 None None None Human 7.3 pEC50 = 7.3 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
11206058 214133 4 None None None Human 4.2 pEC50 = 4.2 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL310360 214133 4 None None None Human 4.2 pEC50 = 4.2 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
127049855 277516 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805220 277516 0 None None None Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25149708 371640 0 None None None Human 8.2 pEC50 = 8.2 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
CHEMBL502339 371640 0 None None None Human 8.2 pEC50 = 8.2 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
58227401 350418 0 None None None Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None None None Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
46887079 22823 0 None None None Human 5.2 pEC50 = 5.2 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094142 22823 0 None None None Human 5.2 pEC50 = 5.2 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
127051301 277488 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25130914 370502 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL492677 370502 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
156015638 352187 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
58227163 350430 0 None None None Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None None None Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25149613 353096 0 None None None Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 353096 0 None None None Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
136773074 313265 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4077914 313265 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
42625221 372712 0 None None None Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 372712 0 None None None Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
24798144 219665 0 None None None Mouse 8.1 pEC50 = 8.1 Binding
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 219665 0 None None None Mouse 8.1 pEC50 = 8.1 Binding
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
10374457 62553 2 None None None Human 5.2 pEC50 = 5.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm030905y
CHEMBL13795 62553 2 None None None Human 5.2 pEC50 = 5.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm030905y
11819221 99037 2 None None None Human 6.1 pEC50 = 6.1 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153061 99037 2 None None None Human 6.1 pEC50 = 6.1 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
1247 7944 80 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1375 7944 80 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
774 7944 80 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL90 7944 80 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
90667229 219040 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 319 7 3 3 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1cccs1 10.1039/C3MD00245D
CHEMBL3220630 219040 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 319 7 3 3 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1cccs1 10.1039/C3MD00245D
11546127 195851 1 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL25725 195851 1 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
182527 220093 3 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL325327 220093 3 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
46887042 23074 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 23074 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
25149521 352953 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 352953 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
155552061 350445 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None None None Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
155517880 350627 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
1249 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
13499360 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
CHEMBL90019 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
1249 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
13499360 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90019 4105 12 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
1247 7944 80 None None None Human 8.0 pEC50 = 8.0 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 7944 80 None None None Human 8.0 pEC50 = 8.0 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 7944 80 None None None Human 8.0 pEC50 = 8.0 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 7944 80 None None None Human 8.0 pEC50 = 8.0 Binding
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
4024 4117 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
9989505 4117 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
CHEMBL82298 4117 17 None None None Human 6.0 pEC50 = 6.0 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
1247 7944 80 None None None Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 7944 80 None None None Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 7944 80 None None None Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 7944 80 None None None Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
16718567 22478 0 None None None Human 9.0 pIC50 = 9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091874 22478 0 None None None Human 9.0 pIC50 = 9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
123886688 450113 0 None None None Human 7.0 pIC50 = 7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 280 2 1 7 0.6 [C-]#[N+]c1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
CHEMBL6011830 450113 0 None None None Human 7.0 pIC50 = 7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 280 2 1 7 0.6 [C-]#[N+]c1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
46885297 22729 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 318 1 1 6 2.5 CN1CCN(c2nc(O)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093438 22729 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 318 1 1 6 2.5 CN1CCN(c2nc(O)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
17747460 124089 14 None None None Human 5.0 pIC50 = 5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 124089 14 None None None Human 5.0 pIC50 = 5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
DB12806 124089 14 None None None Human 5.0 pIC50 = 5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
46884945 22561 0 None None None Human 5.0 pIC50 = 5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 330 1 0 5 3.6 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CC(C)N1C 10.1016/j.bmcl.2010.02.097
CHEMBL1092331 22561 0 None None None Human 5.0 pIC50 = 5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 330 1 0 5 3.6 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CC(C)N1C 10.1016/j.bmcl.2010.02.097
71548501 462495 0 None None None Human 8.0 pIC50 = 8.0 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.4 Cc1nc2c(N3CCN(C)CC3)nc3ncc(Cl)cc3n2n1 nan
CHEMBL6040387 462495 0 None None None Human 8.0 pIC50 = 8.0 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.4 Cc1nc2c(N3CCN(C)CC3)nc3ncc(Cl)cc3n2n1 nan
71547931 366472 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3c3ncnn23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4794724 366472 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3c3ncnn23)C1 10.1021/acs.jmedchem.7b01855
11335478 309062 0 None None None Human 6.0 pIC50 = 6.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115693 309062 0 None None None Human 6.0 pIC50 = 6.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
10660 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None None None Human 5.0 pIC50 = 5.0 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
11709443 22562 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092332 22562 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71548405 355989 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 0 7 1.1 CN(C)C1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782441 355989 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 0 7 1.1 CN(C)C1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
46884998 22293 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 1 1 5 2.6 NC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090532 22293 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 1 1 5 2.6 NC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
25112105 22479 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091875 22479 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
71547681 366319 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4792733 366319 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71547284 372211 10 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
CHEMBL5095103 372211 10 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
71547935 443746 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 329 2 1 7 1.6 Clc1cnc2nc(N3CCNCC3)n3nc(C4CC4)nc3c2c1 nan
CHEMBL5943446 443746 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 329 2 1 7 1.6 Clc1cnc2nc(N3CCNCC3)n3nc(C4CC4)nc3c2c1 nan
71547681 366319 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
CHEMBL4792733 366319 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
71547765 356307 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
CHEMBL4786816 356307 0 None None None Human 6.9 pIC50 = 6.9 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
46885128 22286 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.2 CNC1(C)CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090519 22286 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.2 CNC1(C)CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
46885129 22287 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 1 5 3.2 Clc1ccc2oc3c(N4CC5CCCNC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
CHEMBL1090520 22287 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 1 5 3.2 Clc1ccc2oc3c(N4CC5CCCNC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
46885241 22591 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 2 1 5 3.8 CN[C@@H]1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092543 22591 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 2 1 5 3.8 CN[C@@H]1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
156013896 352155 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
71547937 464857 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ncc(Cl)cc3n3ccnc23)CC1 nan
CHEMBL6064575 464857 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ncc(Cl)cc3n3ccnc23)CC1 nan
71547849 407374 0 None None None Human 7.8 pIC50 = 7.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.4 Cc1nc2c3cc(Cl)cnc3nc(N3CCN(C)CC3)n2n1 nan
CHEMBL5764903 407374 0 None None None Human 7.8 pIC50 = 7.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.4 Cc1nc2c3cc(Cl)cnc3nc(N3CCN(C)CC3)n2n1 nan
89477417 443299 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 332 2 1 6 1.4 CNC1CN(c2nc3ncc(Br)cc3c3ccnn23)C1 nan
CHEMBL5938789 443299 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 332 2 1 6 1.4 CNC1CN(c2nc3ncc(Br)cc3c3ccnn23)C1 nan
16656869 22420 1 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.1 CNC1CCN(c2nc(C)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091559 22420 1 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.1 CNC1CCN(c2nc(C)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
124087 2860 75 None None None Human 4.8 pIC50 = 4.8 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 2860 75 None None None Human 4.8 pIC50 = 4.8 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 2860 75 None None None Human 4.8 pIC50 = 4.8 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 2860 75 None None None Human 4.8 pIC50 = 4.8 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 2860 75 None None None Human 4.8 pIC50 = 4.8 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
11566111 22661 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092933 22661 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71547932 366150 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4790239 366150 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 10.1021/acs.jmedchem.7b01855
13680692 366774 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 313 2 0 8 0.9 CN1CCN(c2nc3ccc([N+](=O)[O-])cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4798729 366774 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 313 2 0 8 0.9 CN1CCN(c2nc3ccc([N+](=O)[O-])cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547932 366150 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 nan
CHEMBL4790239 366150 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 nan
46885239 22510 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092064 22510 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2010.02.097
71547762 366106 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 nan
CHEMBL4789645 366106 0 None None None Human 6.8 pIC50 = 6.8 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 nan
71547762 366106 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4789645 366106 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
2063135 22692 6 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093180 22692 6 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
71548029 425326 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 269 2 1 7 0.4 CNC1CN(c2nc3ncc(C)cc3n3cnnc23)C1 nan
CHEMBL5852641 425326 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 269 2 1 7 0.4 CNC1CN(c2nc3ncc(C)cc3n3cnnc23)C1 nan
11695388 22560 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.2 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CCN1C 10.1016/j.bmcl.2010.02.097
CHEMBL1092330 22560 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.2 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CCN1C 10.1016/j.bmcl.2010.02.097
71548032 410608 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 279 2 1 7 0.1 C#Cc1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
CHEMBL5798362 410608 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 279 2 1 7 0.1 C#Cc1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
9904236 28317 25 None None None Human 5.7 pIC50 = 5.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 28317 25 None None None Human 5.7 pIC50 = 5.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
71547279 450522 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3cnc(Cl)cc3n3cnnc23)C1 nan
CHEMBL6015973 450522 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3cnc(Cl)cc3n3cnnc23)C1 nan
71548124 450798 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 285 3 1 8 0.1 CNC1CN(c2nc3ncc(OC)cc3n3cnnc23)C1 nan
CHEMBL6018904 450798 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 285 3 1 8 0.1 CNC1CN(c2nc3ncc(OC)cc3n3cnnc23)C1 nan
46884997 22040 0 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 0 5 3.2 CN(C)C1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088888 22040 0 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 0 5 3.2 CN(C)C1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1530 4450 49 None None None Human 4.7 pIC50 = 4.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 4450 49 None None None Human 4.7 pIC50 = 4.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 4450 49 None None None Human 4.7 pIC50 = 4.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 4450 49 None None None Human 4.7 pIC50 = 4.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 4450 49 None None None Human 4.7 pIC50 = 4.7 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
20889070 355711 5 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778864 355711 5 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
20889070 355711 5 None None None Human 7.7 pIC50 = 7.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 nan
CHEMBL4778864 355711 5 None None None Human 7.7 pIC50 = 7.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 nan
117661174 406508 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 309 1 1 7 0.8 NC1CN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)C1 nan
CHEMBL5755970 406508 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 309 1 1 7 0.8 NC1CN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)C1 nan
123659754 408439 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 280 1 1 7 0.6 [C-]#[N+]c1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
CHEMBL5775356 408439 0 None None None Human 6.7 pIC50 = 6.7 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 280 1 1 7 0.6 [C-]#[N+]c1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
820836 202991 6 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 268 1 0 6 1.0 CN1CCN(c2nc3ccccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL306316 202991 6 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 268 1 0 6 1.0 CN1CCN(c2nc3ccccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
121237834 294059 0 None None None Human 5.6 pIC50 = 5.6 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL3929465 294059 0 None None None Human 5.6 pIC50 = 5.6 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
71548502 413301 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 361 1 0 7 1.5 Cc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Br nan
CHEMBL5828454 413301 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 361 1 0 7 1.5 Cc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Br nan
46884996 22313 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 Clc1ccc2oc3c(N4CCN5CCCC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
CHEMBL1090655 22313 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 Clc1ccc2oc3c(N4CCN5CCCC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
123202818 410909 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 294 1 0 7 1.0 [C-]#[N+]c1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 nan
CHEMBL5801741 410909 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 294 1 0 7 1.0 [C-]#[N+]c1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 nan
71548223 355699 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778712 355699 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547685 366359 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 294 1 0 8 0.3 CN1CCN(c2nc3ncc(C#N)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4793425 366359 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 294 1 0 8 0.3 CN1CCN(c2nc3ncc(C#N)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548223 355699 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 nan
CHEMBL4778712 355699 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 nan
71548596 448719 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ccc(Cl)nc3n3cnnc23)C1 nan
CHEMBL5996612 448719 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ccc(Cl)nc3n3cnnc23)C1 nan
71548591 461963 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 300 3 1 9 -0.0 CNC1CN(c2nc3ncc([N+](=O)[O-])cc3n3cnnc23)C1 nan
CHEMBL6034828 461963 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 300 3 1 9 -0.0 CNC1CN(c2nc3ncc([N+](=O)[O-])cc3n3cnnc23)C1 nan
71548033 446656 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 281 3 1 7 0.7 C=Cc1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
CHEMBL5974538 446656 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 281 3 1 7 0.7 C=Cc1cnc2nc(N3CC(NC)C3)c3nncn3c2c1 nan
71548410 464205 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 288 2 1 6 1.3 CNC1CN(c2nc3ncc(Cl)cc3n3ccnc23)C1 nan
CHEMBL6057551 464205 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 288 2 1 6 1.3 CNC1CN(c2nc3ncc(Cl)cc3n3ccnc23)C1 nan
71548412 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
71547764 356178 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 328 1 0 8 0.9 CN1CCN(c2nc3nc(C#N)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4784683 356178 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 328 1 0 8 0.9 CN1CCN(c2nc3nc(C#N)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
123807903 462653 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 328 1 0 7 1.6 [C-]#[N+]c1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
CHEMBL6042069 462653 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 328 1 0 7 1.6 [C-]#[N+]c1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
71548498 356067 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4783487 356067 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548498 356067 0 None None None Human 7.6 pIC50 = 7.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 nan
CHEMBL4783487 356067 0 None None None Human 7.6 pIC50 = 7.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 nan
71548031 366283 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4792352 366283 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548031 366283 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 nan
CHEMBL4792352 366283 0 None None None Human 6.6 pIC50 = 6.6 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 nan
16656871 22292 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090531 22292 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1279 7960 58 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
4908365 7960 58 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
CHEMBL129198 7960 58 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
71548412 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
71548319 366586 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 CN1CCCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4796300 366586 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 CN1CCCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
46885178 22033 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 336 2 1 5 3.2 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088859 22033 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 336 2 1 5 3.2 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2010.02.097
71547284 372211 10 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
CHEMBL5095103 372211 10 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
71548224 356347 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 10.1021/acs.jmedchem.7b01855
CHEMBL4787243 356347 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 10.1021/acs.jmedchem.7b01855
71548224 356347 0 None None None Human 6.5 pIC50 = 6.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 nan
CHEMBL4787243 356347 0 None None None Human 6.5 pIC50 = 6.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 nan
71547599 355902 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3ncccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4781409 355902 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3ncccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547680 366207 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3cccnc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4791152 366207 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3cccnc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
11709905 22686 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 342 2 0 5 3.7 CN1CCN(c2nc(C3CC3)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093138 22686 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 342 2 0 5 3.7 CN1CCN(c2nc(C3CC3)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
71548225 412680 0 None None None Human 6.5 pIC50 = 6.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 323 2 1 7 1.4 CNC1CN(c2nc3ncc(Cl)c(Cl)c3n3cnnc23)C1 nan
CHEMBL5821487 412680 0 None None None Human 6.5 pIC50 = 6.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 323 2 1 7 1.4 CNC1CN(c2nc3ncc(Cl)c(Cl)c3n3cnnc23)C1 nan
16656872 22229 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090190 22229 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
71548027 355689 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778591 355689 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548027 355689 0 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 nan
CHEMBL4778591 355689 0 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 nan
71548412 3905 26 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
9879 3905 26 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
CHEMBL4790724 3905 26 None None None Human 7.5 pIC50 = 7.5 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
71547284 372211 10 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
CHEMBL5095103 372211 10 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 1 7 0.8 CNC1CN(c2nc3ncc(Br)cc3n3cnnc23)C1 nan
71548409 462165 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 332 2 1 6 1.4 CNC1CN(c2nc3ncc(Br)cc3n3ccnc23)C1 nan
CHEMBL6036923 462165 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 332 2 1 6 1.4 CNC1CN(c2nc3ncc(Br)cc3n3ccnc23)C1 nan
3934857 22419 32 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.1 Cc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
CHEMBL1091558 22419 32 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.1 Cc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
71547282 366436 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C 10.1021/acs.jmedchem.7b01855
CHEMBL4794336 366436 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C 10.1021/acs.jmedchem.7b01855
71547282 366436 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C nan
CHEMBL4794336 366436 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C nan
71547678 366683 0 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 nan
CHEMBL4797517 366683 0 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 nan
1279 7960 58 None None None Mouse 7.4 pIC50 = 7.4 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 7960 58 None None None Mouse 7.4 pIC50 = 7.4 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 7960 58 None None None Mouse 7.4 pIC50 = 7.4 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
89477685 366908 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 1 7 1.1 CN[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4800462 366908 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 1 7 1.1 CN[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
117660010 425479 0 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 319 0 0 6 1.9 CC1=NC2C(N3CCN(C)CC3)=Nc3ncc(Cl)cc3C2O1 nan
CHEMBL5854302 425479 0 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 319 0 0 6 1.9 CC1=NC2C(N3CCN(C)CC3)=Nc3ncc(Cl)cc3C2O1 nan
89477651 366787 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 10.1021/acs.jmedchem.7b01855
CHEMBL4798915 366787 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 10.1021/acs.jmedchem.7b01855
89477651 366787 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 nan
CHEMBL4798915 366787 0 None None None Human 6.4 pIC50 = 6.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 nan
71548412 3905 26 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
9879 3905 26 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
CHEMBL4790724 3905 26 None None None Human 7.4 pIC50 = 7.4 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br nan
11638468 22662 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1C2CCC1CN(c1ncnc3c1oc1ccc(Cl)cc13)C2 10.1016/j.bmcl.2010.02.097
CHEMBL1092934 22662 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1C2CCC1CN(c1ncnc3c1oc1ccc(Cl)cc13)C2 10.1016/j.bmcl.2010.02.097
71547281 366633 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 2 0 7 1.5 CN(C)[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4796842 366633 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 2 0 7 1.5 CN(C)[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
1267 8287 36 None None None Human 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None None None Human 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None None None Human 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
71547848 366401 0 None None None Human 7.3 pIC50 = 7.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
CHEMBL4793974 366401 0 None None None Human 7.3 pIC50 = 7.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
89477709 366081 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4789385 366081 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
89477709 366081 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 nan
CHEMBL4789385 366081 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 nan
123737866 409092 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 314 2 1 7 1.3 [C-]#[N+]c1nc2nc(N3CC(NC)C3)c3nncn3c2cc1Cl nan
CHEMBL5782119 409092 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 314 2 1 7 1.3 [C-]#[N+]c1nc2nc(N3CC(NC)C3)c3nncn3c2cc1Cl nan
71547597 366491 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 nan
CHEMBL4795091 366491 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 nan
71547597 366491 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4795091 366491 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71548128 426468 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 323 1 1 7 1.4 Clc1cc2c(nc1Cl)nc(N1CCNCC1)c1nncn12 nan
CHEMBL5865056 426468 0 None None None Human 6.3 pIC50 = 6.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 323 1 1 7 1.4 Clc1cc2c(nc1Cl)nc(N1CCNCC1)c1nncn12 nan
71547848 366401 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4793974 366401 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71547765 356307 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl 10.1021/acs.jmedchem.7b01855
CHEMBL4786816 356307 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl 10.1021/acs.jmedchem.7b01855
71547682 356029 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 275 1 1 7 0.5 NC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782945 356029 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 275 1 1 7 0.5 NC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
89477439 355908 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4781484 355908 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 10.1021/acs.jmedchem.7b01855
71515465 355975 0 None None None Human 7.3 pIC50 = 7.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 nan
CHEMBL4782303 355975 0 None None None Human 7.3 pIC50 = 7.3 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 nan
58475282 355499 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 282 1 0 6 1.3 Cc1ccc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4776004 355499 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 282 1 0 6 1.3 Cc1ccc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71548222 431412 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 3 1 8 1.1 CCOc1nc2nc(N3CCNCC3)c3nncn3c2cc1Cl nan
CHEMBL5917477 431412 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 3 1 8 1.1 CCOc1nc2nc(N3CCNCC3)c3nncn3c2cc1Cl nan
71548313 446729 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 373 1 0 7 1.7 Brc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
CHEMBL5975401 446729 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 373 1 0 7 1.7 Brc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
71548126 405885 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 0 8 1.1 COc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
CHEMBL5749759 405885 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 2 0 8 1.1 COc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl nan
71547938 406618 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 288 1 1 6 1.3 Clc1cnc2nc(N3CCNCC3)c3nccn3c2c1 nan
CHEMBL5757167 406618 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 288 1 1 6 1.3 Clc1cnc2nc(N3CCNCC3)c3nccn3c2c1 nan
71548411 356396 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4787983 356396 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548411 356396 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 nan
CHEMBL4787983 356396 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 nan
71548505 426557 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 1 1 6 1.0 CNC1CN(C2=Nc3ncc(Br)cc3N3CCN=C23)C1 nan
CHEMBL5866052 426557 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 334 1 1 6 1.0 CNC1CN(C2=Nc3ncc(Br)cc3N3CCN=C23)C1 nan
53380276 366186 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 0 5 2.3 CN1CCN(c2cc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4790726 366186 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 0 5 2.3 CN1CCN(c2cc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
46885181 22652 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 293 2 1 6 2.0 CNC1CCN(c2ncnc3c2oc2ccc(C#N)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092880 22652 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 293 2 1 6 2.0 CNC1CCN(c2ncnc3c2oc2ccc(C#N)cc23)C1 10.1016/j.bmcl.2010.02.097
89477539 366097 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.9 N[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4789543 366097 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.9 N[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
71548314 406486 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 421 1 0 7 1.6 Ic1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
CHEMBL5755609 406486 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 421 1 0 7 1.6 Ic1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 nan
71515465 355975 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782303 355975 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
89477439 355908 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 nan
CHEMBL4781484 355908 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 nan
71548026 430644 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 381 2 1 7 0.7 CNC1CN(c2nc3ncc(I)cc3n3cnnc23)C1 nan
CHEMBL5909604 430644 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 381 2 1 7 0.7 CNC1CN(c2nc3ncc(I)cc3n3cnnc23)C1 nan
71547761 464357 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 1 1 7 0.8 Brc1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
CHEMBL6058993 464357 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 333 1 1 7 0.8 Brc1cnc2nc(N3CCNCC3)c3nncn3c2c1 nan
71547683 355643 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778068 355643 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547683 355643 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 nan
CHEMBL4778068 355643 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 nan
CHEMBL5087167 479245 0 None None None Mouse 5.2 pIC50 = 5.2 Binding
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 378 2 0 7 3.3 Cn1cc2c(-c3c(-c4ccc(F)cn4)nn4c3COC(C)(C)C4)ccnc2n1 10.6019/CHEMBL5058645
89480010 427147 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 316 1 0 6 1.9 CN1CCN(c2nc3ncc(Cl)cc3c3cn(C)nc23)CC1 nan
CHEMBL5872684 427147 0 None None None Human 7.2 pIC50 = 7.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 316 1 0 6 1.9 CN1CCN(c2nc3ncc(Cl)cc3c3cn(C)nc23)CC1 nan
71548028 447399 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 305 3 1 7 1.0 CNC1CN(c2nc3ncc(C(F)F)cc3n3cnnc23)C1 nan
CHEMBL5982898 447399 0 None None None Human 6.2 pIC50 = 6.2 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 305 3 1 7 1.0 CNC1CN(c2nc3ncc(C(F)F)cc3n3cnnc23)C1 nan
71547850 409120 0 None None None Human 7.1 pIC50 = 7.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 1 7 1.0 Cc1nc2c3cc(Cl)cnc3nc(N3CCNCC3)n2n1 nan
CHEMBL5782392 409120 0 None None None Human 7.1 pIC50 = 7.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 1 7 1.0 Cc1nc2c3cc(Cl)cnc3nc(N3CCNCC3)n2n1 nan
71548226 410784 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 2 1 7 1.2 CNC1CN(c2nc3ncc(Br)c(C)c3n3cnnc23)C1 nan
CHEMBL5800337 410784 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 347 2 1 7 1.2 CNC1CN(c2nc3ncc(Br)c(C)c3n3cnnc23)C1 nan
89477445 355885 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 10.1021/acs.jmedchem.7b01855
CHEMBL4781143 355885 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 10.1021/acs.jmedchem.7b01855
89477445 355885 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 nan
CHEMBL4781143 355885 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 nan
71547678 366683 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4797517 366683 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
24994634 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
Inhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxisInhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
Inhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxisInhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
Inhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxisInhibition of mouse HRH4 in Mouse bone marrow mast cell (mBMMC) using mBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
24994634 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 4374 36 None None None Mouse 8.1 pIC50 = 8.1 Binding
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
11682208 22590 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1092542 22590 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
46885177 22445 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 282 2 1 5 2.5 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091729 22445 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 282 2 1 5 2.5 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C)cc23)C1 10.1016/j.bmcl.2010.02.097
1279 7960 58 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 7960 58 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 7960 58 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
16656874 22422 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091569 22422 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
71548125 406316 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 321 4 1 8 0.7 CNC1CN(c2nc3ncc(OC(F)F)cc3n3cnnc23)C1 nan
CHEMBL5753963 406316 0 None None None Human 6.1 pIC50 = 6.1 Binding
HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.HotSpot Assay: In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofactors were prepared in reaction buffer. Compounds were delivered into the reaction, followed 15-20 minutes later by addition of a mixture of ATP (Sigma, St. Louis Mo.) and 33P ATP (Perkin Elmer, Waltham Mass.) to a final concentration of 10 μM. Reactions were carried out at room temperature for 120 min, followed by spotting of the reaction mixtures onto P81 ion exchange filter paper (Whatman Inc., Piscataway, N.J.). Unbound phosphate was removed by extensive washing of filters in 0.75% phosphoric acid. After subtraction of background derived from control reactions containing inactive enzyme, kinase activity data was expressed as the percent of remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions. IC50 values and curve fits were obtained using Prism (GraphPad Software).Reaction Conditions: Buffer Conditions: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, and 1% DMSO. ATP concentration: 10 μM. Reaction Time: 2 hours. Compound 3 was tested at 10 concentrations as follows with a comparison to the common kinase inhibitor reference compound staurosporine. Compounds were tested in a 10-point IC50 mode with 3-fold serial dilution starting at 10 uM. Control Compound was tested in a 10-point IC50 with 3-fold serial dilution starting at 20 uM.
ChEMBL 321 4 1 8 0.7 CNC1CN(c2nc3ncc(OC(F)F)cc3n3cnnc23)C1 nan
46885298 22730 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 332 2 0 6 2.8 COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
CHEMBL1093439 22730 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 332 2 0 6 2.8 COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
16656870 22041 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CNC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088889 22041 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CNC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1279 7960 58 None 177 2 Human 8.0 pKd = 8 Binding
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
4908365 7960 58 None 177 2 Human 8.0 pKd = 8 Binding
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL129198 7960 58 None 177 2 Human 8.0 pKd = 8 Binding
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
71525681 180557 0 None None None Human 8.0 pKd = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 180557 0 None None None Human 8.0 pKd = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846300 161722 3 None None None Human 8.0 pKd = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None None None Human 8.0 pKd = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
156013896 352155 0 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
2818 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL253391 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 1973 61 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
24994634 4374 36 None -2 3 Human 7.9 pKd = 7.9 Binding
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 4374 36 None -2 3 Human 7.9 pKd = 7.9 Binding
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 4374 36 None -2 3 Human 7.9 pKd = 7.9 Binding
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
11846300 161722 3 None None None Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None None None Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
71519674 180558 0 None None None Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 180558 0 None None None Human 7.9 pKd = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
1247 7944 80 None -81 9 Rat 6.9 pKd = 6.9 Binding
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -81 9 Rat 6.9 pKd = 6.9 Binding
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -81 9 Rat 6.9 pKd = 6.9 Binding
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -81 9 Rat 6.9 pKd = 6.9 Binding
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
135398737 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
2818 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL253391 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 1973 61 None -7 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
155513612 350289 0 None 1 3 Mouse 7.8 pKd = 7.8 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 1 3 Mouse 7.8 pKd = 7.8 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156015638 352187 0 None -147 3 Mouse 6.8 pKd = 6.8 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None -147 3 Mouse 6.8 pKd = 6.8 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
119570 6422 62 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 6422 62 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 6422 62 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 6422 62 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 6422 62 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
1247 7944 80 None -6 9 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 7944 80 None -6 9 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 7944 80 None -6 9 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 7944 80 None -6 9 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
168268716 385305 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 385305 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168268680 385309 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 385309 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168268827 385323 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 385323 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168268853 385329 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 385329 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168273471 385344 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 385344 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273549 385346 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 385346 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168273640 385348 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 385348 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273745 385351 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 385351 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168274129 385352 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 385352 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168275750 385369 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 385369 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
168276867 385378 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 385378 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
168277996 385390 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 385390 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168278471 385392 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 385392 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168278543 385395 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 385395 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168280339 385409 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221885 385409 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168281536 385425 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 385425 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
168281746 385426 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 385426 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
168283097 385437 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 385437 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168283321 385439 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 385439 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168283536 385444 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222074 385444 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
168284289 385450 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 385450 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168284480 385454 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 385454 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
168286141 385469 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 385469 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168286426 385471 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 385471 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290235 385513 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 385513 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168290815 385519 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 385519 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168291233 385525 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 385525 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
168292954 385542 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 385542 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168294161 385551 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 385551 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
168294445 385555 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 385555 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
168294166 385559 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 385559 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
168294449 385563 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 385563 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168294767 385564 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 385564 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294770 385565 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 385565 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
168294776 385570 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 385570 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
168295528 385575 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 385575 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294178 385579 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 385579 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168295541 385583 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 385583 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295543 385584 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 385584 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168295803 385588 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 385588 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168294182 385590 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 385590 0 None -5 4 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
156013896 352155 0 None -8 3 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156015638 352187 0 None -147 3 Mouse 6.8 pKd = 6.8 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None -147 3 Mouse 6.8 pKd = 6.8 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 350289 0 None 1 3 Mouse 7.8 pKd = 7.8 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 1 3 Mouse 7.8 pKd = 7.8 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -8 3 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
2818 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL253391 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 1973 61 None -7 4 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
71525679 180555 0 None None None Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 180555 0 None None None Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
155513612 350289 0 None -1 3 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -1 3 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -1 3 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -1 3 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
11846300 161722 3 None None None Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None None None Human 7.7 pKd = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
24745335 607 14 None None None Human 7.6 pKd = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 607 14 None None None Human 7.6 pKd = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 607 14 None None None Human 7.6 pKd = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 607 14 None None None Human 7.6 pKd = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
1279 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
4908365 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
CHEMBL129198 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
1223 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
2790 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
CHEMBL14690 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
1223 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
2790 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
CHEMBL14690 1963 35 None -194 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
156013896 352155 0 None -22 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 350289 0 None 1 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 1 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None 1 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 1 3 Mouse 7.5 pKd = 7.5 Binding
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -1 3 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -1 3 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -1 3 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -1 3 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -2 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -2 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -8 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
56835171 141988 0 None None None Human 7.4 pKd = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL1935574 141988 0 None None None Human 7.4 pKd = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
155513612 350289 0 None -2 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -2 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -8 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 7.4 pKd = 7.4 Binding
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -25 9 Mouse 7.4 pKd = 7.4 Binding
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -25 9 Mouse 7.4 pKd = 7.4 Binding
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -25 9 Mouse 7.4 pKd = 7.4 Binding
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -25 9 Mouse 7.4 pKd = 7.4 Binding
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -22 3 Mouse 7.3 pKd = 7.3 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.3 pKd = 7.3 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -6 9 Human 8.3 pKd = 8.3 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 7944 80 None -6 9 Human 8.3 pKd = 8.3 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 7944 80 None -6 9 Human 8.3 pKd = 8.3 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 7944 80 None -6 9 Human 8.3 pKd = 8.3 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -22 3 Mouse 7.3 pKd = 7.3 Binding
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.3 pKd = 7.3 Binding
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 350289 0 None -2 3 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -2 3 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 350289 0 None -2 3 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -2 3 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156013896 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156013896 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -22 3 Mouse 7.2 pKd = 7.2 Binding
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
2818 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL253391 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 1973 61 None -7 4 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
11846300 161722 3 None None None Human 7.1 pKd = 7.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None None None Human 7.1 pKd = 7.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
156015638 352187 0 None -72 3 Human 7.1 pKd = 7.1 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None -72 3 Human 7.1 pKd = 7.1 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156015638 352187 0 None -72 3 Human 7.1 pKd = 7.1 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None -72 3 Human 7.1 pKd = 7.1 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
71525678 180554 0 None None None Human 8.1 pKd = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 180554 0 None None None Human 8.1 pKd = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
156013896 352155 0 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
54587788 124293 0 None None None Human 10.4 pKi = 10.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 4 3 5 1.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770975 124293 0 None None None Human 10.4 pKi = 10.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 4 3 5 1.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
23653543 140320 0 None None None Human 10.0 pKi = 10 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914541 140320 0 None None None Human 10.0 pKi = 10 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
54587787 124289 0 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770971 124289 0 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
46235428 20934 0 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 20934 0 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
54586763 124286 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 3 2 5 1.9 CN1CCN(c2cc(N)nc(NCC(C)(C)C)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770968 124286 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 3 2 5 1.9 CN1CCN(c2cc(N)nc(NCC(C)(C)C)c2)CC1 10.1016/j.bmcl.2011.03.017
24826169 140312 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914462 140312 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
16718567 22478 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1091874 22478 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
66816027 442475 0 None None None Human 9.3 pKi = 9.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 328 4 2 4 3.4 CN[C@@H]1CCN(c2ccnc(N[C@@H]3C[C@@H]4C[C@H]([C@H]3C)C4(C)C)c2)C1 nan
CHEMBL5949302 442475 0 None None None Human 9.3 pKi = 9.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 328 4 2 4 3.4 CN[C@@H]1CCN(c2ccnc(N[C@@H]3C[C@@H]4C[C@H]([C@H]3C)C4(C)C)c2)C1 nan
24737950 140402 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 361 2 2 6 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914781 140402 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 361 2 2 6 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
58227148 235988 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 235988 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
57399746 140377 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914755 140377 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)CC1 10.1016/j.bmcl.2011.08.014
54580885 124291 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 4 3 5 1.8 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770973 124291 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 4 3 5 1.8 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
24826766 135881 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914750 135881 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
59777338 219668 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236556 219668 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
58227342 235975 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 nan
CHEMBL3393534 235975 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 nan
58227259 235997 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 nan
CHEMBL3393556 235997 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 nan
44517823 430952 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 328 4 2 4 3.4 CN[C@@H]1CCN(c2ccnc(N[C@H]3C[C@H]4C[C@@H]([C@@H]3C)C4(C)C)c2)C1 nan
CHEMBL5912704 430952 0 None None None Human 9.0 pKi = 9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 328 4 2 4 3.4 CN[C@@H]1CCN(c2ccnc(N[C@H]3C[C@H]4C[C@@H]([C@@H]3C)C4(C)C)c2)C1 nan
1247 7944 80 None -12 11 Human 9.0 pKi = 9 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
1375 7944 80 None -12 11 Human 9.0 pKi = 9 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
774 7944 80 None -12 11 Human 9.0 pKi = 9 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
CHEMBL90 7944 80 None -12 11 Human 9.0 pKi = 9 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
1223 1963 35 None -21 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
54581940 124310 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770992 124310 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
24797598 124320 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1771001 124320 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
11224088 273896 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1021/jm800876b
CHEMBL373579 273896 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1021/jm800876b
24798144 219665 0 None 18 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3236553 219665 0 None 18 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
58227342 235975 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393534 235975 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
11224088 273896 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
CHEMBL373579 273896 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
24825998 140382 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914760 140382 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)CC1 10.1016/j.bmcl.2011.08.014
57396301 140404 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 2.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914783 140404 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 2.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2011.08.014
127050310 278107 0 None None None Human 9.0 pKi = 9 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 347 3 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(C(C)(F)F)cc23)C1 10.1039/C6MD00108D
CHEMBL3819260 278107 0 None None None Human 9.0 pKi = 9 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 347 3 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(C(C)(F)F)cc23)C1 10.1039/C6MD00108D
46222048 23293 0 None -4 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1098230 23293 0 None -4 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
24994542 219666 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236554 219666 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
24948752 140319 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.4 Nc1nc(N2CCCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914540 140319 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.4 Nc1nc(N2CCCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
24825727 140321 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914542 140321 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
46222048 23293 0 None -4 2 Human 9.0 pKi = 9.0 Binding
Inhibition of human recombinant histamine H4 receptor expressed in CHO cellsInhibition of human recombinant histamine H4 receptor expressed in CHO cells
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098230 23293 0 None -4 2 Human 9.0 pKi = 9.0 Binding
Inhibition of human recombinant histamine H4 receptor expressed in CHO cellsInhibition of human recombinant histamine H4 receptor expressed in CHO cells
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
155524115 350512 0 None -2 3 Human 8.9 pKi = 8.9 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 350512 0 None -2 3 Human 8.9 pKi = 8.9 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
24798144 219665 0 None 18 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 219665 0 None 18 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
155524115 350512 0 None 1 3 Mouse 8.9 pKi = 8.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 350512 0 None 1 3 Mouse 8.9 pKi = 8.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
24797604 219664 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
CHEMBL3236552 219664 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
44231618 20221 0 None 1 4 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1079516 20221 0 None 1 4 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
25128824 385707 0 None 3 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 385707 0 None 3 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
24992077 219683 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236571 219683 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
44231618 20221 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1079516 20221 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
44129130 432014 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 432014 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1223 1963 35 None -21 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
44187557 390404 0 None 3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL553423 390404 0 None 3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1247 7944 80 None -12 11 Human 8.8 pKi = 8.8 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
1375 7944 80 None -12 11 Human 8.8 pKi = 8.8 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
774 7944 80 None -12 11 Human 8.8 pKi = 8.8 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
CHEMBL90 7944 80 None -12 11 Human 8.8 pKi = 8.8 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
11957573 4107 26 None -7 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
1250 4107 26 None -7 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
3692 4107 26 None -7 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
CHEMBL19439 4107 26 None -7 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
44547268 235967 0 None None None Human 8.8 pKi = 8.8 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 nan
CHEMBL3393526 235967 0 None None None Human 8.8 pKi = 8.8 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 nan
16202258 140489 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915536 140489 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
66740859 219691 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 327 3 2 5 2.3 CN[C@@H]1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236579 219691 0 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 327 3 2 5 2.3 CN[C@@H]1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)C1 10.1021/jm401727m
24798232 219672 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 1.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236560 219672 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 1.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCCN[C@H]3C2)n1 10.1021/jm401727m
44231735 22104 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089390 22104 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
25129527 370651 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL493720 370651 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
135353337 445809 0 None None None Human 8.0 pKi = 8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 414 5 1 6 4.2 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(F)(F)F)cc1C1CCC1 nan
CHEMBL5965464 445809 0 None None None Human 8.0 pKi = 8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 414 5 1 6 4.2 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(F)(F)F)cc1C1CCC1 nan
25217643 221657 0 None None None Human 8.0 pKi = 8 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
CHEMBL3290570 221657 0 None None None Human 8.0 pKi = 8 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
135525668 140483 0 None 263 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915348 140483 0 None 263 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
25217643 221657 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysis
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290570 221657 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysis
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
1249 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10176414 8813 16 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 8813 16 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 8813 16 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10060212 469434 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72769 469434 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681807 180475 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 8 3 8 1.6 CC(C)CCc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375668 180475 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 8 3 8 1.6 CC(C)CCc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681804 180500 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1ccnc(N)n1)c1cc(-c2ccccc2)nc(N)n1 10.1021/jm301886t
CHEMBL2375770 180500 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1ccnc(N)n1)c1cc(-c2ccccc2)nc(N)n1 10.1021/jm301886t
1223 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
1223 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
1249 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
13499360 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL90019 4105 12 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
53233802 124305 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770987 124305 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
70692529 157348 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 303 2 1 2 2.7 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047466 157348 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 303 2 1 2 2.7 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
46228994 430932 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 466 6 1 7 2.7 CC1CCCCN1S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591249 430932 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 466 6 1 7 2.7 CC1CCCCN1S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
1223 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
2790 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
CHEMBL14690 1963 35 None -21 8 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
45268092 392554 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 352 6 3 3 3.6 N=C(NCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560111 392554 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 352 6 3 3 3.6 N=C(NCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45268093 392555 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 400 6 3 3 3.4 N=C(NCc1ccc(I)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560112 392555 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 400 6 3 3 3.4 N=C(NCc1ccc(I)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45267230 393431 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL563342 393431 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
24737954 140400 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(F)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914778 140400 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(F)c23)C1 10.1016/j.bmcl.2011.08.014
24826522 140407 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914786 140407 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
24826168 140410 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914789 140410 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24745335 607 14 None 6 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 607 14 None 6 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 607 14 None 6 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 607 14 None 6 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
71525680 180560 0 None 97 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 284 3 2 6 1.3 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376806 180560 0 None 97 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 284 3 2 6 1.3 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
71525678 180554 0 None 4 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 180554 0 None 4 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25101945 385646 0 None -3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 385646 0 None -3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
136192886 119279 0 None -1 4 Mouse 7.0 pKi = 7 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632411 119279 0 None -1 4 Mouse 7.0 pKi = 7 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
44129134 431638 0 None -22 2 Rat 7.0 pKi = 7 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 431638 0 None -22 2 Rat 7.0 pKi = 7 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11694543 157464 2 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204843 157464 2 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
11521414 278531 1 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 2 2 2.7 c1nc(CCCCNC2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL383324 278531 1 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 2 2 2.7 c1nc(CCCCNC2CCCCC2)c[nH]1 10.1021/jm0504353
9812843 470101 1 None -4 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2011.06.123
CHEMBL78838 470101 1 None -4 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2011.06.123
53233904 124283 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770965 124283 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
39732699 157345 1 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 1 2 2 1.4 O=C(c1cc2cccc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047463 157345 1 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 1 2 2 1.4 O=C(c1cc2cccc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
70696623 157353 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 2 2 2 2.0 CNC1CN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047471 157353 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 2 2 2 2.0 CNC1CN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
51354298 121671 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 233 4 1 4 1.9 CC(C)(C)c1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688944 121671 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 233 4 1 4 1.9 CC(C)(C)c1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
45267237 392883 0 None -7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 7 3 3 3.2 Cc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL561451 392883 0 None -7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 7 3 3 3.2 Cc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
53378933 219685 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 269 3 2 5 1.2 Nc1nc(Cc2ccccc2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236573 219685 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 269 3 2 5 1.2 Nc1nc(Cc2ccccc2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
11087453 157309 1 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL2047270 157309 1 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1039/C2MD20212C
44395335 139349 0 None 25 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 266 4 2 3 1.5 CN(C)CCNC(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL187210 139349 0 None 25 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 266 4 2 3 1.5 CN(C)CCNC(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
10978141 19489 0 None -4 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 19489 0 None -4 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
71681477 180487 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 398 7 4 8 3.3 Nc1nc(NCCNc2cc(-c3ccccc3)nc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375758 180487 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 398 7 4 8 3.3 Nc1nc(NCCNc2cc(-c3ccccc3)nc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
71681802 180498 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1cc(NCCNc2ccnc(N)n2)ncn1 10.1021/jm301886t
CHEMBL2375769 180498 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1cc(NCCNc2ccnc(N)n2)ncn1 10.1021/jm301886t
206876 42802 4 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL128637 42802 4 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
66572107 157304 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
CHEMBL2047265 157304 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
66572115 157324 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047442 157324 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
11469514 213887 0 None -64 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL309654 213887 0 None -64 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
46890591 21354 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 436 6 1 4 4.8 Cc1cc(OCCCN2CC3CCCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084811 21354 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 436 6 1 4 4.8 Cc1cc(OCCCN2CC3CCCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227158 235990 0 None None None Human 5.0 pKi = 5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 nan
CHEMBL3393549 235990 0 None None None Human 5.0 pKi = 5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 nan
44275807 193705 0 None -12302 10 Human 5.0 pKi = 5 Binding
Binding affinity towards human histaminergic (H4) receptorBinding affinity towards human histaminergic (H4) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 193705 0 None -12302 10 Human 5.0 pKi = 5 Binding
Binding affinity towards human histaminergic (H4) receptorBinding affinity towards human histaminergic (H4) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
4242418 236279 9 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL339826 236279 9 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
71681978 180482 0 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 310 5 3 5 1.7 CN(CCNc1ccnc(N)n1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm301886t
CHEMBL2375753 180482 0 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 310 5 3 5 1.7 CN(CCNc1ccnc(N)n1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm301886t
58227158 235990 0 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393549 235990 0 None None None Human 5.0 pKi = 5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 10.1016/j.bmcl.2014.12.027
72901200 238494 30 None -6918 33 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL3480577 238494 30 None -6918 33 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL4552554 478323 0 None -1 2 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 407 5 1 3 3.2 O=C(c1ccc(F)cc1)N1CC(COc2ccc(Br)cc2)(C(=O)O)C1 10.6019/CHEMBL4507298
135353505 410063 0 None None None Human 6.0 pKi = 6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 384 6 1 8 2.2 CCc1cc(S(C)(=O)=O)ccc1N(Cc1ccncn1)c1ccnc(N)n1 nan
CHEMBL5792345 410063 0 None None None Human 6.0 pKi = 6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 384 6 1 8 2.2 CCc1cc(S(C)(=O)=O)ccc1N(Cc1ccncn1)c1ccnc(N)n1 nan
135353282 408146 0 None None None Human 7.0 pKi = 7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 505 6 1 7 4.7 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cccc(C(F)(F)F)n1)c1ccnc(N)n1 nan
CHEMBL5772631 408146 0 None None None Human 7.0 pKi = 7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 505 6 1 7 4.7 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cccc(C(F)(F)F)n1)c1ccnc(N)n1 nan
57391926 142148 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938967 142148 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
11846300 161722 3 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL213912 161722 3 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
135353347 409675 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 343 6 1 7 3.2 CCOc1cc(F)ccc1N(Cc1coc(C)n1)c1ccnc(N)n1 nan
CHEMBL5788203 409675 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 343 6 1 7 3.2 CCOc1cc(F)ccc1N(Cc1coc(C)n1)c1ccnc(N)n1 nan
24854583 196476 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 304 2 0 4 3.0 CN1CCN(c2nc3ccccc3nc2-c2ccccc2)CC1 10.1021/jm7014217
CHEMBL260372 196476 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 304 2 0 4 3.0 CN1CCN(c2nc3ccccc3nc2-c2ccccc2)CC1 10.1021/jm7014217
16082860 270517 0 None -7 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL377572 270517 0 None -7 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
57391032 140372 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@H]3C[C@@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914749 140372 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@H]3C[C@@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25179297 347908 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL453877 347908 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
24759518 353202 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL473302 353202 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178342 370049 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489070 370049 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179297 347908 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL453877 347908 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25178342 370049 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489070 370049 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
71518535 177364 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 1 5 2.6 CN1CCN(c2nc(N(C)C)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314763 177364 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 1 5 2.6 CN1CCN(c2nc(N(C)C)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
10978141 19489 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL105803 19489 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
57393730 140156 0 None -1905 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910386 140156 0 None -1905 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
24826681 140390 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914768 140390 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
127049855 277516 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805220 277516 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
57391869 125837 0 None -19 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789349 125837 0 None -19 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
90645163 221677 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1cc(C)cc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
CHEMBL3290590 221677 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1cc(C)cc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
10656971 40309 3 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL123137 40309 3 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2011.07.114
121238070 331304 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4278404 331304 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
25178555 348297 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454891 348297 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178555 348297 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454891 348297 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
155540201 347028 0 None -42 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
CHEMBL4516173 347028 0 None -42 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
1279 7960 58 None -281 7 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -281 7 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -281 7 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
832283 26667 5 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL118572 26667 5 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
832283 26667 5 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL118572 26667 5 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
10269628 276071 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 355 1 0 4 4.6 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL377985 276071 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 355 1 0 4 4.6 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
54582866 124306 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(N)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770988 124306 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(N)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2011.03.017
25133970 370822 1 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL494679 370822 1 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
49841962 141976 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3c(-c4ccoc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935562 141976 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3c(-c4ccoc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
44547568 235971 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393530 235971 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
13731320 314517 0 None None None Human 6.0 pKi = 6.0 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 2 2 2 4.0 O=C(Nc1cccc2ccccc12)N1CCC(c2c[nH]cn2)CC1 10.1016/j.ejmech.2016.09.074
CHEMBL4092578 314517 0 None None None Human 6.0 pKi = 6.0 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 2 2 2 4.0 O=C(Nc1cccc2ccccc12)N1CCC(c2c[nH]cn2)CC1 10.1016/j.ejmech.2016.09.074
127035837 274820 0 None -5 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753334 274820 0 None -5 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
21842421 221658 1 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 270 2 1 6 0.9 CN1CCN(c2nc(N)nc(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290571 221658 1 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 270 2 1 6 0.9 CN1CCN(c2nc(N)nc(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2014.06.032
10688021 312035 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 332 8 1 3 4.3 O=C(/C=C/c1ccccc1)c1ccc(OCCCc2c[nH]cn2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4063170 312035 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 332 8 1 3 4.3 O=C(/C=C/c1ccccc1)c1ccc(OCCCc2c[nH]cn2)cc1 10.1016/j.ejmech.2016.09.074
9944571 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL338937 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
135350663 444069 0 None None None Human 8.0 pKi = 8.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 286 4 1 4 3.8 C/C=C/c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5946892 444069 0 None None None Human 8.0 pKi = 8.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 286 4 1 4 3.8 C/C=C/c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
135353290 464334 0 None None None Human 8.0 pKi = 8.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 5 1 5 4.3 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1OCC(F)(F)F nan
CHEMBL6058736 464334 0 None None None Human 8.0 pKi = 8.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 5 1 5 4.3 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1OCC(F)(F)F nan
9944571 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL338937 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0341047
23650961 8371 34 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
9276 8371 34 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
CHEMBL3301609 8371 34 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
DB12522 8371 34 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
24803710 296995 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 400 6 2 5 4.1 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(F)c(F)ccc2[nH]1 nan
CHEMBL3953011 296995 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 400 6 2 5 4.1 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(F)c(F)ccc2[nH]1 nan
25101945 385646 0 None -3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 385646 0 None -3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
118720437 234848 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 275 3 2 5 1.0 CN[C@@H]1CCN(c2cc(CC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354811 234848 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 275 3 2 5 1.0 CN[C@@H]1CCN(c2cc(CC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
24737952 140405 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(OC)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914784 140405 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(OC)cc23)C1 10.1016/j.bmcl.2011.08.014
9944571 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338937 235882 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
24996854 219676 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
CHEMBL3236564 219676 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
71603142 180550 0 None 54 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 3 2 5 1.2 CCc1ccc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376796 180550 0 None 54 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 3 2 5 1.2 CCc1ccc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
44129282 429400 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)cc(Cl)c3n2)CC1 10.1021/jm901379s
CHEMBL589746 429400 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)cc(Cl)c3n2)CC1 10.1021/jm901379s
71603139 180547 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 2 2 5 1.5 Nc1nc(N2CCNCC2)c2ccc(C3CC3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL2376793 180547 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 2 2 5 1.5 Nc1nc(N2CCNCC2)c2ccc(C3CC3)cc2n1 10.1016/j.bmcl.2013.02.091
45257132 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155513612 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
44450493 196872 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 1 1 4 1.3 CN1CCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL262859 196872 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 1 1 4 1.3 CN1CCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
1279 7960 58 None -4 7 Mouse 7.9 pKi = 7.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -4 7 Mouse 7.9 pKi = 7.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -4 7 Mouse 7.9 pKi = 7.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
126963283 309061 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115677 309061 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
10660 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None -77 13 Human 5.0 pKi = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1241 4169 46 None 1 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
3614 4169 46 None 1 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
CHEMBL507 4169 46 None 1 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
135353304 409161 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 6 1 7 3.3 CCS(=O)(=O)c1ccc(N(c2ccnc(N)n2)C(C)C)c(OC(F)(F)F)c1 nan
CHEMBL5782882 409161 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 6 1 7 3.3 CCS(=O)(=O)c1ccc(N(c2ccnc(N)n2)C(C)C)c(OC(F)(F)F)c1 nan
49841609 141970 15 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3c(Br)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935556 141970 15 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3c(Br)cccc23)CC1 10.1016/j.bmcl.2011.10.104
51354871 121689 0 None -22 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 290 6 0 4 3.3 c1c(CC2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
CHEMBL1688982 121689 0 None -22 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 290 6 0 4 3.3 c1c(CC2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
164618508 369213 0 None -363 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4869194 369213 0 None -363 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
164620678 369299 0 None -177 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4870510 369299 0 None -177 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
58227159 350354 0 None 47 2 Human 6.9 pKi = 6.9 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 1 5 1.7 CN1CCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4595907 350354 0 None 47 2 Human 6.9 pKi = 6.9 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 1 5 1.7 CN1CCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
122193099 251972 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 374 3 1 6 2.1 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Br)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628046 251972 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 374 3 1 6 2.1 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Br)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
51354008 121666 0 None -3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 253 5 1 4 1.8 c1ccc(Cc2cn(CCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688939 121666 0 None -3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 253 5 1 4 1.8 c1ccc(Cc2cn(CCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
51354586 121686 0 None -15 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 2.9 CC(c1cn(CCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
CHEMBL1688978 121686 0 None -15 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 2.9 CC(c1cn(CCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
16082824 159531 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL209598 159531 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
54585778 124307 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(N)nc(NCCO)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770989 124307 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(N)nc(NCCO)n2)CC1 10.1016/j.bmcl.2011.03.017
58227165 235977 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393536 235977 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
24853664 196687 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261517 196687 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
10773349 22407 1 None -11 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 22407 1 None -11 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10715857 156684 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 398 8 1 3 3.5 O=C(CCCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL20338 156684 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 398 8 1 3 3.5 O=C(CCCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
16082820 161577 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213250 161577 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
10776393 19831 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 239 7 2 3 2.1 CC[C@H](C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1076267 19831 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 239 7 2 3 2.1 CC[C@H](C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
118725542 235978 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393537 235978 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
1279 7960 58 None -3 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 7960 58 None -3 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 7960 58 None -3 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
90645161 221675 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3cc(F)cc(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290588 221675 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3cc(F)cc(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
135350850 448987 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 338 6 1 5 3.9 CCOc1cc(F)ccc1N(Cc1ccccc1)c1ccnc(N)n1 nan
CHEMBL5999642 448987 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 338 6 1 5 3.9 CCOc1cc(F)ccc1N(Cc1ccccc1)c1ccnc(N)n1 nan
135353336 451389 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 7 1 7 4.5 CC(C)Cc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6025213 451389 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 7 1 7 4.5 CC(C)Cc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353361 463486 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 451 5 1 5 6.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncccc1Cl)c1ccnc(N)n1 nan
CHEMBL6050277 463486 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 451 5 1 5 6.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncccc1Cl)c1ccnc(N)n1 nan
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
45257132 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
24994635 219682 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236570 219682 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
24826442 140378 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1ccc2oc3c(N4CCN(C)CC4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1914756 140378 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1ccc2oc3c(N4CCN(C)CC4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
155513612 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
58227402 432241 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 233 4 2 5 0.7 c1cc(N2CCNCC2)nc(NCC2CC2)n1 nan
CHEMBL5925766 432241 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 233 4 2 5 0.7 c1cc(N2CCNCC2)nc(NCC2CC2)n1 nan
1226 4125 18 None 2 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
41376 4125 18 None 2 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
CHEMBL12608 4125 18 None 2 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
24745335 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
71603135 180543 0 None 26 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 2 2 5 2.3 Nc1nc(N2CCNCC2)c2ccc(C3CCCC3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL2376789 180543 0 None 26 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 2 2 5 2.3 Nc1nc(N2CCNCC2)c2ccc(C3CCCC3)cc2n1 10.1016/j.bmcl.2013.02.091
71525589 180561 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 286 3 2 6 1.5 CN[C@@H]1CCN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376807 180561 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 286 3 2 6 1.5 CN[C@@H]1CCN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
24745335 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 607 14 None -6 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
3035746 371399 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL498770 371399 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
155513612 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 350289 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
1249 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
13499360 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90019 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1253 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10023327 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
10023327 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
10023327 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
1253 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
132937 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL19010 4209 4 None -9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
11065080 43286 1 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL129488 43286 1 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
66573460 157333 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.2 Cc1cc(Cl)cc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047451 157333 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.2 Cc1cc(Cl)cc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
21638785 371849 3 None -4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL503605 371849 3 None -4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
44129132 431840 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 6 1 7 1.3 CN1CCN(c2nc(NCCS(=O)(=O)N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592188 431840 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 6 1 7 1.3 CN1CCN(c2nc(NCCS(=O)(=O)N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10176414 8813 16 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
1246 8813 16 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL281576 8813 16 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
45267233 388183 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 304 7 3 4 2.8 COc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL541171 388183 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 304 7 3 4 2.8 COc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1249 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
13499360 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90019 4105 12 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
25128823 385260 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 385260 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
135350590 428421 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 6 2.7 C=C(C)c1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
CHEMBL5887486 428421 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 6 2.7 C=C(C)c1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
127050431 277603 0 None 4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 277603 0 None 4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11451949 140317 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 384 6 1 4 3.9 CN1CCN(CCCOc2ccc(-c3nc4cc(Cl)ccc4[nH]3)cc2)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914533 140317 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 384 6 1 4 3.9 CN1CCN(CCCOc2ccc(-c3nc4cc(Cl)ccc4[nH]3)cc2)CC1 10.1016/j.bmcl.2011.08.014
46228126 466162 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.4 CN1CCN(c2cc(NCc3ccc(C(F)(F)F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL612131 466162 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.4 CN1CCN(c2cc(NCc3ccc(C(F)(F)F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
60150166 348762 0 None -75 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
CHEMBL4560123 348762 0 None -75 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
168295543 385584 0 None -56 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 385584 0 None -56 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
164610648 368147 0 None -120 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4852212 368147 0 None -120 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
10820930 20131 0 None 1 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL107877 20131 0 None 1 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
24826443 140392 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914770 140392 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
10800875 20610 0 None -75 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1081718 20610 0 None -75 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
24745335 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 607 14 None -30 5 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
1223 1963 35 None -165 8 Mouse 6.9 pKi = 6.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -165 8 Mouse 6.9 pKi = 6.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -165 8 Mouse 6.9 pKi = 6.9 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
10800875 20610 0 None -75 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1081718 20610 0 None -75 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
11206058 214133 4 None -10 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL310360 214133 4 None -10 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
1267 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3035905 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
CHEMBL260374 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3062060 24668 2 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 221 4 6 3 -1.0 N=C(N)NCc1cccc(CNC(=N)N)n1 10.1021/jm7014777
CHEMBL1162346 24668 2 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 221 4 6 3 -1.0 N=C(N)NCc1cccc(CNC(=N)N)n1 10.1021/jm7014777
135353325 411951 0 None None None Human 5.9 pKi = 5.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 378 6 1 7 3.6 CCOc1cc(F)ccc1N(Cc1cn2ccccc2n1)c1ccnc(N)n1 nan
CHEMBL5813588 411951 0 None None None Human 5.9 pKi = 5.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 378 6 1 7 3.6 CCOc1cc(F)ccc1N(Cc1cn2ccccc2n1)c1ccnc(N)n1 nan
11511026 39926 0 None -208 4 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
CHEMBL1223683 39926 0 None -208 4 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
1267 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
3035905 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
CHEMBL260374 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
10106063 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
CHEMBL321860 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
24826000 140414 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 2 2 6 3.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914793 140414 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 2 2 6 3.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)C1 10.1016/j.bmcl.2011.08.014
1267 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
3035905 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
CHEMBL260374 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
1279 7960 58 None -4 7 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -4 7 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -4 7 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10106063 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321860 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
9974306 469376 0 None 12 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 469376 0 None 12 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
56849569 143840 0 None -77 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 381 7 2 4 4.4 N#Cc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963332 143840 0 None -77 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 381 7 2 4 4.4 N#Cc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11499453 157869 0 None -79 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205834 157869 0 None -79 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
11672850 158322 3 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206451 158322 3 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
1267 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
3035905 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
CHEMBL260374 8287 36 None -28 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
10106063 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321860 212979 11 None 16 2 Human 6.9 pKi = 6.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
5310982 194029 1 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 194029 1 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
71681975 180479 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 296 5 4 5 1.4 Nc1nccc(NCCNC(=O)c2cc3ccccc3[nH]2)n1 10.1021/jm301886t
CHEMBL2375750 180479 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 296 5 4 5 1.4 Nc1nccc(NCCNC(=O)c2cc3ccccc3[nH]2)n1 10.1021/jm301886t
71681642 180494 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1nc(NCCNc2ccnc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375765 180494 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1nc(NCCNc2ccnc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
11286909 470140 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL79126 470140 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
10678661 19698 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 19698 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11043445 116511 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 116511 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
168294449 385563 0 None -645 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 385563 0 None -645 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
66572111 157310 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 1 3 1.8 CC(=O)c1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL2047271 157310 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 1 3 1.8 CC(=O)c1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
118720435 234847 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 225 3 2 5 0.3 CN[C@@H]1CCN(c2cc(CF)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354809 234847 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 225 3 2 5 0.3 CN[C@@H]1CCN(c2cc(CF)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
90645151 221659 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290572 221659 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2014.06.032
16082833 161802 0 None -23 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214312 161802 0 None -23 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
54584826 124311 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770993 124311 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
57395538 140482 0 None 151 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915347 140482 0 None 151 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
57395538 140482 0 None 151 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915347 140482 0 None 151 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
25178343 337106 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL448962 337106 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178343 337106 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL448962 337106 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
57403269 140388 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 1 6 2.5 CN1CCN(c2nc(N)nc3c4cc(Cl)ccc4[s+]([O-])c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914766 140388 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 1 6 2.5 CN1CCN(c2nc(N)nc3c4cc(Cl)ccc4[s+]([O-])c23)CC1 10.1016/j.bmcl.2011.08.014
24854705 196465 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 321 3 0 6 2.6 CN1CCN(c2nc3ccccc3nc2Oc2cccnc2)CC1 10.1021/jm7014217
CHEMBL260274 196465 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 321 3 0 6 2.6 CN1CCN(c2nc3ccccc3nc2Oc2cccnc2)CC1 10.1021/jm7014217
164619208 368950 0 None -446 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
CHEMBL4864852 368950 0 None -446 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
10678661 19698 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 19698 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
57402929 142113 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938844 142113 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
135353324 443395 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 453 6 1 8 3.9 Nc1nccc(N(Cc2cocn2)c2ccc(S(=O)(=O)C(F)(F)F)cc2C2CCC2)n1 nan
CHEMBL5939813 443395 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 453 6 1 8 3.9 Nc1nccc(N(Cc2cocn2)c2ccc(S(=O)(=O)C(F)(F)F)cc2C2CCC2)n1 nan
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
57392827 140394 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914772 140394 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
58227163 350430 0 None 40 2 Human 7.9 pKi = 7.9 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 350430 0 None 40 2 Human 7.9 pKi = 7.9 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
1375 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
774 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL90 7944 80 None -12 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
16082856 155184 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL215628 155184 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
46929647 40642 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243394 40642 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
11858011 314858 0 None None None Human 4.9 pKi = 4.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 9 0 3 4.6 O=C(c1ccccc1)c1ccc(OCCCCCN2CCCC2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4096444 314858 0 None None None Human 4.9 pKi = 4.9 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 9 0 3 4.6 O=C(c1ccccc1)c1ccc(OCCCCCN2CCCC2)cc1 10.1016/j.ejmech.2016.09.074
16352 236038 7 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 236038 7 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
11240759 214910 1 None -190 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL311473 214910 1 None -190 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
24853662 196430 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 326 3 0 5 3.1 CN1CCN(c2nc3ccccc3nc2OC2CCCCC2)CC1 10.1021/jm7014217
CHEMBL260043 196430 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 326 3 0 5 3.1 CN1CCN(c2nc3ccccc3nc2OC2CCCCC2)CC1 10.1021/jm7014217
54584378 125875 0 None -50 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789782 125875 0 None -50 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164626153 369648 0 None -6456 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 369648 0 None -6456 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
54583874 124304 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N)nc(N3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770986 124304 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N)nc(N3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
54584378 125875 0 None -50 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789782 125875 0 None -50 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
135353311 446845 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 376 7 1 7 2.5 COCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
CHEMBL5976921 446845 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 376 7 1 7 2.5 COCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
46890122 21693 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 421 9 2 5 4.3 Cc1cc(OCCCNCCc2cn(C)cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086344 21693 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 421 9 2 5 4.3 Cc1cc(OCCCNCCc2cn(C)cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
155568016 350011 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 264 4 1 6 1.1 CCC(CC)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4590367 350011 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 264 4 1 6 1.1 CCC(CC)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
135350832 463207 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 7 3.3 C/C=C/c1cc(C#N)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6047313 463207 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 7 3.3 C/C=C/c1cc(C#N)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353345 463444 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 6 1 6 2.9 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)CC)cc1C1CC1 nan
CHEMBL6049767 463444 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 6 1 6 2.9 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)CC)cc1C1CC1 nan
58227319 235981 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393540 235981 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
56849571 143841 0 None -117 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 401 8 2 5 4.5 O=[N+]([O-])c1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963347 143841 0 None -117 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 401 8 2 5 4.5 O=[N+]([O-])c1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
25179126 347510 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm800876b
CHEMBL452849 347510 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm800876b
25179126 347510 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm901379s
CHEMBL452849 347510 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm901379s
164609729 368398 0 None -2187 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 368398 0 None -2187 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164622886 369223 0 None -131 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4869389 369223 0 None -131 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164626509 369605 0 None -3 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4874969 369605 0 None -3 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
11043445 116511 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL1632410 116511 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
1247 7944 80 None -74 11 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 7944 80 None -74 11 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 7944 80 None -74 11 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 7944 80 None -74 11 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
11609325 38438 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 312 1 1 3 2.3 CN1CCN(C(=O)c2nc3c(Cl)cc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL120221 38438 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 312 1 1 3 2.3 CN1CCN(C(=O)c2nc3c(Cl)cc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
24825796 140367 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 NC[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914744 140367 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 NC[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
46228100 444767 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 315 4 1 6 2.1 CN1CCN(c2cc(SCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595413 444767 0 None None None Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 315 4 1 6 2.1 CN1CCN(c2cc(SCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
58227302 464762 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 219 3 2 5 0.6 N[C@@H]1CCN(c2ccnc(NC3CC3)n2)C1 nan
CHEMBL6063639 464762 0 None None None Human 6.9 pKi = 6.9 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 219 3 2 5 0.6 N[C@@H]1CCN(c2ccnc(NC3CC3)n2)C1 nan
44628631 140395 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3c(Cl)cc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914773 140395 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3c(Cl)cc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
71525679 180555 0 None -15 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 180555 0 None -15 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
4060730 43234 34 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL129199 43234 34 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
24853594 196491 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 348 4 0 5 3.3 Cc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL260470 196491 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 348 4 0 5 3.3 Cc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
44414495 161479 0 None -34 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 5 0 2 6.3 CC1CC(C)CN(Cc2ccc(-c3ccc(CN4CC(C)CC(C)C4)cc3)cc2)C1 10.1016/j.bmc.2008.10.029
CHEMBL212869 161479 0 None -34 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 5 0 2 6.3 CC1CC(C)CN(Cc2ccc(-c3ccc(CN4CC(C)CC(C)C4)cc3)cc2)C1 10.1016/j.bmc.2008.10.029
127026017 274761 0 None -12 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752972 274761 0 None -12 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
164614907 367893 0 None -436 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848697 367893 0 None -436 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
57390263 140458 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 330 1 2 7 1.8 Nc1nc(N2CC3CCNC3C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915052 140458 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 330 1 2 7 1.8 Nc1nc(N2CC3CCNC3C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
9900313 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129444 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1007/s00044-004-0106-7
135353272 413810 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cnco1)c1ccnc(N)n1 nan
CHEMBL5833662 413810 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cnco1)c1ccnc(N)n1 nan
135353378 429334 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 393 7 1 7 4.2 CCCc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5896737 429334 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 393 7 1 7 4.2 CCCc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353274 451410 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ccon1)c1ccnc(N)n1 nan
CHEMBL6025409 451410 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ccon1)c1ccnc(N)n1 nan
137395032 463541 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 424 5 2 5 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1n[nH]cc1F)c1ccnc(N)n1 nan
CHEMBL6050794 463541 0 None None None Human 7.9 pKi = 7.9 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 424 5 2 5 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1n[nH]cc1F)c1ccnc(N)n1 nan
9900313 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129444 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0341047
1279 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 7960 58 None -3 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
46890592 20722 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 20722 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
9900313 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129444 43276 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
156013896 352155 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 352155 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
25129523 370534 40 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 370534 40 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
1249 4105 12 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
13499360 4105 12 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
CHEMBL90019 4105 12 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
1247 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1375 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
774 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
137655927 314748 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 403 7 2 3 5.2 O=C(NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL4095224 314748 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 403 7 2 3 5.2 O=C(NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
71603141 180549 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 2 2 5 1.2 CCc1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376795 180549 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 2 2 5 1.2 CCc1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
54585779 124309 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770991 124309 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
25179303 365949 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 5 2.6 CNc1nc(N2CCN3CCCC3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL512568 365949 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 5 2.6 CNc1nc(N2CCN3CCCC3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
51354304 121680 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCn2cc(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688972 121680 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCn2cc(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
71519016 177346 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 322 2 2 5 2.3 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314501 177346 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 322 2 2 5 2.3 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
71518859 177372 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 294 2 3 5 1.6 Nc1nc(N2CCNCC2)c2cc(-c3ccccc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314772 177372 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 294 2 3 5 1.6 Nc1nc(N2CCNCC2)c2cc(-c3ccccc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
156014317 352192 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 575 10 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/C=C/c3ccc(N(C)C)cc3)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4650854 352192 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 575 10 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/C=C/c3ccc(N(C)C)cc3)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
11724853 197343 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm051008s
CHEMBL266723 197343 0 None -19 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm051008s
57398985 140155 0 None -66 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910385 140155 0 None -66 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
118725539 235964 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 2 0 4 1.8 CN1CCN(c2ccnc(N3CCCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393523 235964 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 2 0 4 1.8 CN1CCN(c2ccnc(N3CCCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
16082822 161441 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@@H]2C[C@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL212705 161441 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@@H]2C[C@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
46228160 443865 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 308 3 0 6 1.6 CN1CCN(c2ncnc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594468 443865 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 308 3 0 6 1.6 CN1CCN(c2ncnc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
2306318 177884 10 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1039/C5MD00022J
CHEMBL232421 177884 10 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1039/C5MD00022J
127036980 274750 0 None -16 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752885 274750 0 None -16 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
57391033 140391 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 287 1 2 6 1.5 Nc1nc(N2CCNCC2)c2oc3cccc(F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914769 140391 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 287 1 2 6 1.5 Nc1nc(N2CCNCC2)c2oc3cccc(F)c3c2n1 10.1016/j.bmcl.2011.08.014
1237 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
156615 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
CHEMBL268229 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
24797248 443894 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594490 443894 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
9951970 19835 0 None -81 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 267 9 2 3 3.0 CCCCC[C@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1076300 19835 0 None -81 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 267 9 2 3 3.0 CCCCC[C@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
121238066 331507 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 3 2 8 -1.0 CN1CCN(c2nc(N)nc(CN3C(=O)NC(C)(C)C3=O)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4282283 331507 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 3 2 8 -1.0 CN1CCN(c2nc(N)nc(CN3C(=O)NC(C)(C)C3=O)n2)CC1 10.1016/j.ejmech.2017.09.035
137395033 411794 0 None None None Human 5.8 pKi = 5.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 2 7 2.1 CCOc1cc(F)ccc1N(Cc1nnc[nH]1)c1ccnc(N)n1 nan
CHEMBL5811710 411794 0 None None None Human 5.8 pKi = 5.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 2 7 2.1 CCOc1cc(F)ccc1N(Cc1nnc[nH]1)c1ccnc(N)n1 nan
10860228 235718 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0341047
CHEMBL338001 235718 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0341047
10860228 235718 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338001 235718 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0502081
3840250 274047 13 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 5 2.4 Cc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
CHEMBL3739776 274047 13 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 5 2.4 Cc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
56851447 143853 0 None -144 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 424 7 2 3 5.9 Clc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1963433 143853 0 None -144 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 424 7 2 3 5.9 Clc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
90645157 221671 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 334 3 1 7 1.5 COc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1Cl 10.1016/j.ejmech.2014.06.032
CHEMBL3290584 221671 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 334 3 1 7 1.5 COc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1Cl 10.1016/j.ejmech.2014.06.032
2971762 385754 4 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL523617 385754 4 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
44450401 312055 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 3 2 4 2.0 O=c1[nH]c2ccc(Cl)cc2nc1NCN1CCCC1 10.1021/jm7014217
CHEMBL406345 312055 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 3 2 4 2.0 O=c1[nH]c2ccc(Cl)cc2nc1NCN1CCCC1 10.1021/jm7014217
2971762 385754 4 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL523617 385754 4 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
164622190 368905 0 None -93 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4864067 368905 0 None -93 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
54586762 124285 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 4 2 5 2.0 CN1CCN(c2cc(N)nc(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770967 124285 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 4 2 5 2.0 CN1CCN(c2cc(N)nc(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2011.03.017
136066109 447401 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
46231557 447401 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
CHEMBL598291 447401 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
5477514 24667 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 408 4 4 5 2.6 C/N=C(\N)N/N=C(/C)c1ccc2sc3ccc(/C(C)=N\N/C(N)=N/C)cc3c2c1 10.1021/jm7014777
CHEMBL1162345 24667 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 408 4 4 5 2.6 C/N=C(\N)N/N=C(/C)c1ccc2sc3ccc(/C(C)=N\N/C(N)=N/C)cc3c2c1 10.1021/jm7014777
24826083 140418 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914797 140418 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
10988959 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL340740 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
4906599 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL436381 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
135350584 412503 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 295 5 1 5 3.4 CCCc1cc(C#N)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5819495 412503 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 295 5 1 5 3.4 CCCc1cc(C#N)ccc1N(c1ccnc(N)n1)C(C)C nan
135353276 444530 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
CHEMBL5951482 444530 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
67087450 235991 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 nan
CHEMBL3393550 235991 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 nan
10988959 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL340740 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0341047
4906599 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL436381 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0341047
57391819 141984 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 361 3 1 6 2.8 CC(=O)c1cccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935570 141984 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 361 3 1 6 2.8 CC(=O)c1cccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)c1 10.1016/j.bmcl.2011.10.104
53233801 124303 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770985 124303 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
10988959 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL340740 236934 2 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
4906599 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL436381 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
71519674 180558 0 None -2 5 Mouse 7.8 pKi = 7.8 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 180558 0 None -2 5 Mouse 7.8 pKi = 7.8 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
56835171 141988 0 None 1 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL1935574 141988 0 None 1 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
71603138 180546 0 None 32 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 2 5 1.9 CNC1CN(c2nc(N)nc3cc(C(C)(C)C)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376792 180546 0 None 32 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 2 5 1.9 CNC1CN(c2nc(N)nc3cc(C(C)(C)C)ccc23)C1 10.1016/j.bmcl.2013.02.091
25128822 370716 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 370716 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
44129214 429431 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 538 7 2 7 3.7 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Br)c(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL589782 429431 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 538 7 2 7 3.7 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Br)c(Cl)cc3n2)CC1 10.1021/jm901379s
136192874 119282 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25147772 347506 9 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 347506 9 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
136192874 119282 0 None -1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None -1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
1375 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
774 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
CHEMBL90 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
1223 1963 35 None -21 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
1247 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
1375 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
774 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL90 7944 80 None -12 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
1279 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
4908365 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
CHEMBL129198 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
10967174 43294 1 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129540 43294 1 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70681963 157352 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 321 2 1 2 2.9 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047470 157352 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 321 2 1 2 2.9 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
4906599 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL436381 333322 9 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1279 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
4908365 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
CHEMBL129198 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
3035746 371399 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL498770 371399 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
45269820 390145 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL551790 390145 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1279 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
4908365 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
CHEMBL129198 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
155491015 350461 6 None -15 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 350461 6 None -15 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
25129525 370817 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1039/C2MD20212C
CHEMBL494648 370817 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1039/C2MD20212C
46228125 444588 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595215 444588 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890020 21688 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 8 3 4 4.5 Cc1cc(OCCCNCC2CCCCN2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086327 21688 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 8 3 4 4.5 Cc1cc(OCCCNCC2CCCCN2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
42641407 430703 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(Cl)cc(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL591013 430703 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(Cl)cc(Cl)cc3n2)CC1 10.1021/jm901379s
127036981 274853 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753621 274853 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
135570464 352998 1 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 278 1 1 5 1.7 CN1CCN(c2nc(O)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL471712 352998 1 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 278 1 1 5 1.7 CN1CCN(c2nc(O)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354297 121670 0 None -5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 289 6 1 6 0.4 CN1CCN(Cc2cn(CCCc3c[nH]cn3)nn2)CC1 10.1021/jm1013488
CHEMBL1688943 121670 0 None -5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 289 6 1 6 0.4 CN1CCN(Cc2cn(CCCc3c[nH]cn3)nn2)CC1 10.1021/jm1013488
46890074 20933 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 403 8 1 3 6.2 Cc1cc(OCCCCCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083160 20933 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 403 8 1 3 6.2 Cc1cc(OCCCCCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
10107667 125881 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789800 125881 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
25178755 350831 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 5 2.6 CNc1nc(N2CCN3CCC[C@H]3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL461537 350831 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 5 2.6 CNc1nc(N2CCN3CCC[C@H]3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
24759518 353202 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL473302 353202 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1267 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
118720439 234854 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 246 2 2 4 2.2 Nc1nc(C2CCCC2)cc(C2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354817 234854 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 246 2 2 4 2.2 Nc1nc(C2CCCC2)cc(C2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
24853527 332209 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 363 4 0 6 3.2 CN1CCN(c2nc3ccccc3nc2Oc2cccc(N(C)C)c2)CC1 10.1021/jm7014217
CHEMBL429691 332209 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 363 4 0 6 3.2 CN1CCN(c2nc3ccccc3nc2Oc2cccc(N(C)C)c2)CC1 10.1021/jm7014217
10107667 125881 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789800 125881 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
10760516 125888 0 None -9 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789829 125888 0 None -9 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
135353360 444220 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 438 6 1 8 3.0 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ccncn1)c1ccnc(N)n1 nan
CHEMBL5948263 444220 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 438 6 1 8 3.0 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ccncn1)c1ccnc(N)n1 nan
127050431 277603 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 277603 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
10760516 125888 0 None -9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789829 125888 0 None -9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
57391034 140415 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914794 140415 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
57396299 140380 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 1 1 6 2.0 CN1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914758 140380 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 1 1 6 2.0 CN1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)CC1 10.1016/j.bmcl.2011.08.014
57396300 140397 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 305 1 2 6 1.6 Nc1nc(N2CCNCC2)c2oc3ccc(F)c(F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914775 140397 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 305 1 2 6 1.6 Nc1nc(N2CCNCC2)c2oc3ccc(F)c(F)c3c2n1 10.1016/j.bmcl.2011.08.014
46228161 444075 13 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 233 1 2 6 -0.3 CN1CCN(c2nc(N)nc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594694 444075 13 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 233 1 2 6 -0.3 CN1CCN(c2nc(N)nc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
1223 1963 35 None -165 8 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -165 8 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -165 8 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
10023327 333639 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11615601 156688 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203390 156688 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
11600849 277826 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL381074 277826 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
66572108 157305 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3c(O)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047266 157305 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3c(O)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
9965450 157311 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3ccc(Cl)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047272 157311 2 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3ccc(Cl)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
45268970 392821 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 318 8 3 4 2.9 COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL561369 392821 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 318 8 3 4 2.9 COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
45267238 392911 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 345 7 4 2 3.5 N=C(NC=C(c1ccccc1)c1ccccc1)NCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL561651 392911 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 345 7 4 2 3.5 N=C(NC=C(c1ccccc1)c1ccccc1)NCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1247 7944 80 None -12 11 Human 6.8 pKi = 6.8 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 6.8 pKi = 6.8 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 6.8 pKi = 6.8 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 6.8 pKi = 6.8 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
127050019 270582 0 None None None Human 6.8 pKi = 6.8 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 233 2 2 5 0.3 CN[C@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1039/C6MD00108D
CHEMBL3818355 270582 0 None None None Human 6.8 pKi = 6.8 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 233 2 2 5 0.3 CN[C@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1039/C6MD00108D
1194 95 1 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 95 1 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 95 1 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
127035835 274690 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 274690 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
70690368 157343 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 1 1 2 2.3 Cc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047461 157343 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 1 1 2 2.3 Cc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24854707 196643 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 338 3 0 5 3.3 CN1CCN(c2nc3ccccc3nc2Oc2ccc(F)cc2)CC1 10.1021/jm7014217
CHEMBL261222 196643 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 338 3 0 5 3.3 CN1CCN(c2nc3ccccc3nc2Oc2ccc(F)cc2)CC1 10.1021/jm7014217
56678756 137927 8 None None None Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL4507280
CHEMBL1834199 137927 8 None None None Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL4507280
57390224 140149 0 None -20 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910379 140149 0 None -20 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
4905344 78813 6 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2cc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1016/j.ejmech.2012.06.016
CHEMBL1437043 78813 6 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2cc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1016/j.ejmech.2012.06.016
70690367 157341 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 287 2 1 3 2.0 COc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047459 157341 0 None None None Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 287 2 1 3 2.0 COc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
59777309 219694 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 2 2 5 0.3 CN[C@@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1021/jm401727m
CHEMBL3236581 219694 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 2 2 5 0.3 CN[C@@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1021/jm401727m
135353346 430775 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 379 6 1 7 3.8 CCc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5910922 430775 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 379 6 1 7 3.8 CCc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353315 432404 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 406 5 2 5 5.1 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cc[nH]n1)c1ccnc(N)n1 nan
CHEMBL5927348 432404 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 406 5 2 5 5.1 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cc[nH]n1)c1ccnc(N)n1 nan
135353340 444945 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 7 1 8 3.9 CC(C)Cc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5956093 444945 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 7 1 8 3.9 CC(C)Cc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353273 445396 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 440 5 2 5 5.7 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1n[nH]cc1Cl)c1ccnc(N)n1 nan
CHEMBL5960823 445396 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 440 5 2 5 5.7 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1n[nH]cc1Cl)c1ccnc(N)n1 nan
57400777 140480 0 None 426 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915345 140480 0 None 426 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
56835171 141988 0 None 1 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 141988 0 None 1 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
3035746 371399 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL498770 371399 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
53378928 234849 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 289 4 2 5 1.4 CN[C@@H]1CCN(c2cc(CCC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354812 234849 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 289 4 2 5 1.4 CN[C@@H]1CCN(c2cc(CCC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
44547564 235972 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 2.2 CN1CCN(c2ccnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393531 235972 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 2.2 CN1CCN(c2ccnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
57400777 140480 0 None 426 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915345 140480 0 None 426 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400738 140455 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.5 Nc1nc(N2CC[C@@H](N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915049 140455 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.5 Nc1nc(N2CC[C@@H](N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
56851445 143869 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 8 2 3 3.8 CCCCN/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963551 143869 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 8 2 3 3.8 CCCCN/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
71603194 180551 0 None 35 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 3 2 5 1.6 CCc1ccc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376797 180551 0 None 35 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 3 2 5 1.6 CCc1ccc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
45257133 444104 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 444104 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
135353318 426020 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ccno1)c1ccnc(N)n1 nan
CHEMBL5859950 426020 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ccno1)c1ccnc(N)n1 nan
155540438 337059 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4483783 337059 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
57394625 140588 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 325 7 2 6 1.7 COc1ccccc1Cn1ccc(NCCc2cnc[nH]2)nc1=O 10.1016/j.bmcl.2011.07.114
CHEMBL1916493 140588 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 325 7 2 6 1.7 COc1ccccc1Cn1ccc(NCCc2cnc[nH]2)nc1=O 10.1016/j.bmcl.2011.07.114
124087 2860 75 None -9120 15 Human 4.8 pKi = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 2860 75 None -9120 15 Human 4.8 pKi = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 2860 75 None -9120 15 Human 4.8 pKi = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 2860 75 None -9120 15 Human 4.8 pKi = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 2860 75 None -9120 15 Human 4.8 pKi = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
137395035 425821 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 398 6 2 7 2.8 CS(=O)(=O)c1ccc(N(Cc2ccn[nH]2)c2ccnc(N)n2)c(C2CCC2)c1 nan
CHEMBL5857967 425821 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 398 6 2 7 2.8 CS(=O)(=O)c1ccc(N(Cc2ccn[nH]2)c2ccnc(N)n2)c(C2CCC2)c1 nan
54587791 124301 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770983 124301 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
10515050 20579 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCCC(C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1081541 20579 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCCC(C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
73355143 182667 0 None -22 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 323 8 2 4 2.8 O=C(NCCOc1ccccc1Cl)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL2413362 182667 0 None -22 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 323 8 2 4 2.8 O=C(NCCOc1ccccc1Cl)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
56678756 137927 8 None None None Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL4507280
CHEMBL1834199 137927 8 None None None Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL4507280
56678756 137927 8 None None None Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL5212743
CHEMBL1834199 137927 8 None None None Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 10.6019/CHEMBL5212743
137634349 311941 0 None -741 2 Human 4.8 pKi = 4.8 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 6 0 3 4.7 CC(=O)c1ccc(OCc2ccc(CN3CCCC(C)C3)cc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4062122 311941 0 None -741 2 Human 4.8 pKi = 4.8 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 6 0 3 4.7 CC(=O)c1ccc(OCc2ccc(CN3CCCC(C)C3)cc2)cc1 10.1016/j.ejmech.2016.09.074
164626370 369741 0 None -14 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4876799 369741 0 None -14 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
155568977 350120 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 281 6 3 3 2.6 c1ccc2[nH]c(CNCC[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
CHEMBL4592695 350120 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 281 6 3 3 2.6 c1ccc2[nH]c(CNCC[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
1237 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.6019/CHEMBL5442175
156615 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.6019/CHEMBL5442175
CHEMBL268229 7956 17 None -676 3 Human 6.8 pKi = 6.8 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.6019/CHEMBL5442175
24854706 196335 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm7014217
CHEMBL259536 196335 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm7014217
1279 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
4908365 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
CHEMBL129198 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
135350874 431411 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 310 3 1 4 3.9 Cc1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5917470 431411 0 None None None Human 7.8 pKi = 7.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 310 3 1 4 3.9 Cc1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
46929554 40638 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243367 40638 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
4060730 43234 34 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL129199 43234 34 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
49841608 141979 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935565 141979 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.10.104
1279 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
4908365 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
CHEMBL129198 7960 58 None -3 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
4060730 43234 34 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129199 43234 34 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
45379805 430930 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 438 6 1 7 1.9 CN1CCN(c2nc(NCCS(=O)(=O)N3CCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591248 430930 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 438 6 1 7 1.9 CN1CCN(c2nc(NCCS(=O)(=O)N3CCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
135353293 430575 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 399 6 1 8 3.1 CS(=O)(=O)c1ccc(N(Cc2cocn2)c2ccnc(N)n2)c(C2CCC2)c1 nan
CHEMBL5908765 430575 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 399 6 1 8 3.1 CS(=O)(=O)c1ccc(N(Cc2cocn2)c2ccnc(N)n2)c(C2CCC2)c1 nan
164585473 367871 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to H4 receptor (unknown origin)Binding affinity to H4 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 367871 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to H4 receptor (unknown origin)Binding affinity to H4 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
71519177 177361 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.9 Nc1nc(N2CC[C@@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314760 177361 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.9 Nc1nc(N2CC[C@@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
112936262 274681 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752195 274681 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
1403136 354383 7 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL475331 354383 7 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm901379s
164611143 368025 0 None -75 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
CHEMBL4850448 368025 0 None -75 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
137646744 313707 0 None None None Human 6.8 pKi = 6.8 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 391 10 1 5 3.0 O=C(CCNC(=O)C(Cc1ccccc1)Cn1ccnc1)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4083336 313707 0 None None None Human 6.8 pKi = 6.8 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 391 10 1 5 3.0 O=C(CCNC(=O)C(Cc1ccccc1)Cn1ccnc1)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
56835171 141988 0 None -14 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from rat H4RDisplacement of [3H]histamine from rat H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 141988 0 None -14 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from rat H4RDisplacement of [3H]histamine from rat H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
90645149 221661 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 284 2 1 6 1.2 Cc1cccc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
CHEMBL3290574 221661 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 284 2 1 6 1.2 Cc1cccc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
135353271 449920 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 330 4 1 5 3.6 CC(C)N(c1ccnc(N)n1)c1ccc(F)cc1OC(F)(F)F nan
CHEMBL6009440 449920 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 330 4 1 5 3.6 CC(C)N(c1ccnc(N)n1)c1ccc(F)cc1OC(F)(F)F nan
46890021 21689 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.8 Cc1cc(OCCCNCC2CCCCN2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086328 21689 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.8 Cc1cc(OCCCNCC2CCCCN2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
135350571 427009 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 350 6 2 7 2.5 C/C=C/c1cc(C(N)=O)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5871117 427009 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 350 6 2 7 2.5 C/C=C/c1cc(C(N)=O)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
118725541 235969 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 1 4 2.0 CCCCNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393528 235969 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 1 4 2.0 CCCCNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
16082858 161551 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL213133 161551 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
45379809 430719 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 420 5 1 8 2.1 CN1CCN(c2nc(NCCN3C(=O)CSC3=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591027 430719 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 420 5 1 8 2.1 CN1CCN(c2nc(NCCN3C(=O)CSC3=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
135398737 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
2818 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL253391 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 1973 61 None -57 61 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
10575070 140153 0 None -79 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910383 140153 0 None -79 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
164622330 369145 0 None -724 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 369145 0 None -724 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
1267 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
3035905 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
CHEMBL260374 8287 36 None -28 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
122193098 251971 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628045 251971 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645162 221676 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 324 2 1 6 1.3 CN1CCN(c2nc(N)nc(-c3cc(F)c(F)c(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290589 221676 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 324 2 1 6 1.3 CN1CCN(c2nc(N)nc(-c3cc(F)c(F)c(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
135350649 405554 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 320 5 1 6 2.2 CCc1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
CHEMBL5746753 405554 0 None None None Human 6.8 pKi = 6.8 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 320 5 1 6 2.2 CCc1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
24745507 140491 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915538 140491 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
45257133 444104 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 444104 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
24826165 140385 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914763 140385 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)CC1 10.1016/j.bmcl.2011.08.014
25109291 366002 9 None -478 12 Human 7.7 pKi = 7.7 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.6019/CHEMBL5442175
CHEMBL519240 366002 9 None -478 12 Human 7.7 pKi = 7.7 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.6019/CHEMBL5442175
1279 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
4908365 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
CHEMBL129198 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
3032915 39388 20 None -1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm0341047
CHEMBL12160 39388 20 None -1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm0341047
127052294 277590 0 None 5 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 277590 0 None 5 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
57394550 140387 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 2 1 7 2.2 COc1ccc2c(c1)sc1c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.08.014
CHEMBL1914765 140387 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 2 1 7 2.2 COc1ccc2c(c1)sc1c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.08.014
51354009 121667 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 267 6 1 4 2.2 c1ccc(Cc2cn(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688940 121667 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 267 6 1 4 2.2 c1ccc(Cc2cn(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
156011119 351076 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 841 18 4 6 8.7 Cc1cc(OCCCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6ccc[nH]6)n5[B-]4(F)F)C=C3)cc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4633688 351076 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 841 18 4 6 8.7 Cc1cc(OCCCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6ccc[nH]6)n5[B-]4(F)F)C=C3)cc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
51354296 121669 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 274 6 1 5 1.6 c1nc(CCCn2cc(CN3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688942 121669 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 274 6 1 5 1.6 c1nc(CCCn2cc(CN3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
1237 7956 17 None -676 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
156615 7956 17 None -676 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
CHEMBL268229 7956 17 None -676 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
756701 443559 29 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 218 1 1 5 0.1 CN1CCN(c2ncnc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594152 443559 29 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 218 1 1 5 0.1 CN1CCN(c2ncnc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
63868328 348309 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4549015 348309 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
58227381 350579 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597817 350579 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
25128822 370716 0 None -10 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 370716 0 None -10 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
25179124 348291 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm800876b
CHEMBL454883 348291 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm800876b
25179122 385798 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL523941 385798 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179124 348291 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm901379s
CHEMBL454883 348291 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm901379s
25179122 385798 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL523941 385798 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1265 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
6422124 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
CHEMBL14638 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
24994634 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
24994634 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
8984 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL3236549 4374 36 None -35 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL4520788 478301 14 None -89 26 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
CHEMBL4520788 478301 14 None -89 26 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
54581937 124281 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 3 1 5 1.3 CC(C)N(C)c1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770963 124281 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 3 1 5 1.3 CC(C)N(C)c1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
137646939 313627 0 None None None Human 7.7 pKi = 7.7 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 335 5 3 4 3.6 CC(C)(CN=C(c1ccccc1O)c1ccccc1O)c1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL4082297 313627 0 None None None Human 7.7 pKi = 7.7 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 335 5 3 4 3.6 CC(C)(CN=C(c1ccccc1O)c1ccccc1O)c1c[nH]cn1 10.1016/j.ejmech.2016.09.074
9878733 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL338051 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
135350664 462191 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 293 4 1 5 3.5 C/C=C/c1cc(C#N)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL6037243 462191 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 293 4 1 5 3.5 C/C=C/c1cc(C#N)ccc1N(c1ccnc(N)n1)C(C)C nan
9878733 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL338051 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0341047
49841610 141980 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3cc(-c4ccccc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935566 141980 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3cc(-c4ccccc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
44547127 234853 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
44547127 234853 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354816 234853 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354816 234853 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
24739219 140325 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 289 1 2 6 1.8 Nc1nc(N2CC(N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914546 140325 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 289 1 2 6 1.8 Nc1nc(N2CC(N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
24826265 140383 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.3 CN1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914761 140383 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.3 CN1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)CC1 10.1016/j.bmcl.2011.08.014
9992865 233442 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL333220 233442 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
9878733 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338051 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
2063135 22692 6 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093180 22692 6 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
44129213 430681 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)c(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL590995 430681 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)c(Cl)cc3n2)CC1 10.1021/jm901379s
71525681 180557 0 None -3 6 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 180557 0 None -3 6 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
136141537 119280 6 None 2 3 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None 2 3 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136030655 119281 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1279 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
4908365 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL129198 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
1251 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1251 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
3035842 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL18661 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1251 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
3035842 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
CHEMBL18661 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
11673377 276585 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 263 7 2 2 3.2 Clc1ccc(CNCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
CHEMBL379027 276585 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 263 7 2 2 3.2 Clc1ccc(CNCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
25129523 370534 40 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 370534 40 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
66572114 157315 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047276 157315 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70690369 157355 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 1 2 2 2.0 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047473 157355 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 1 2 2 2.0 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
9878733 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL338051 235727 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1247 7944 80 None -12 11 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
1375 7944 80 None -12 11 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
774 7944 80 None -12 11 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
CHEMBL90 7944 80 None -12 11 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
1279 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 7960 58 None -3 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
11846298 276604 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
CHEMBL379102 276604 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
155538989 350298 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 3 5 2.1 CC(C)(C)CNc1nccc(NC2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595438 350298 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 3 5 2.1 CC(C)(C)CNc1nccc(NC2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
164608815 367764 0 None -47 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 367764 0 None -47 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4520788 478301 14 None -89 26 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
164611342 368388 0 None -416 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 368388 0 None -416 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
155513612 350289 0 None -69 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -69 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156015838 352161 0 None -2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 373 7 1 2 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650622 352161 0 None -2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 373 7 1 2 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
127036982 274870 0 None -3 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3753784 274870 0 None -3 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
57393769 140441 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 281 1 2 6 1.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915030 140441 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 281 1 2 6 1.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
11688307 142149 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938968 142149 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136141537 119280 6 None -10 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None -10 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
44395364 139187 0 None 15 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186456 139187 0 None 15 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
10037650 19547 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 19547 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
135398737 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
2818 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
38 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
722 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
CHEMBL253391 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
CHEMBL42 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
DB00363 1973 61 None -57 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
11572015 156698 0 None -50 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL203441 156698 0 None -50 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
11600780 157708 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 6 2 2 1.7 CC(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205732 157708 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 6 2 2 1.7 CC(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
1408942 137423 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 254 2 0 4 1.9 CN1CCN(c2cc(-c3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL1824046 137423 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 254 2 0 4 1.9 CN1CCN(c2cc(-c3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.06.123
4060730 43234 34 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 43234 34 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
25129527 370651 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL493720 370651 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
66573462 157335 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 2 2 2 2.2 CNC1CN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047453 157335 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 2 2 2 2.2 CNC1CN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
767246 196373 5 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 242 1 0 4 1.7 Cc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL259745 196373 5 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 242 1 0 4 1.7 Cc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
155550732 350592 0 None -794 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4597895 350592 0 None -794 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
11313837 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
11313837 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1254 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL175782 5081 11 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
71681480 180490 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 307 6 3 7 2.0 Nc1nc(NCCNc2ccncn2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375761 180490 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 307 6 3 7 2.0 Nc1nc(NCCNc2ccncn2)cc(-c2ccccc2)n1 10.1021/jm301886t
57392460 142112 0 None 14 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL1938843 142112 0 None 14 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572104 157301 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ccncc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047262 157301 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ccncc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572112 157313 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3ccc([N+](=O)[O-])cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047274 157313 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3ccc([N+](=O)[O-])cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
44395361 139228 0 None None None Human 4.7 pKi = 4.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 293 1 2 3 2.0 CN1CCN(C(=O)Nc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186640 139228 0 None None None Human 4.7 pKi = 4.7 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 293 1 2 3 2.0 CN1CCN(C(=O)Nc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
10879463 19627 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106570 19627 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10945113 212986 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 212986 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
127035836 274921 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754176 274921 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
164618283 367853 0 None -537 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848026 367853 0 None -537 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
58227326 235983 0 None None None Human 8.7 pKi = 8.7 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 nan
CHEMBL3393542 235983 0 None None None Human 8.7 pKi = 8.7 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 nan
53233805 124282 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770964 124282 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
54585781 124319 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1771000 124319 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
118720442 234856 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 3 5 1.4 Nc1cc(N2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354820 234856 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 3 5 1.4 Nc1cc(N2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
44547268 235967 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393526 235967 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227255 235980 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393539 235980 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
58227252 235985 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393544 235985 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
25112105 22479 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1091875 22479 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24737949 140403 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914782 140403 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
24825996 140409 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914788 140409 0 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
59777341 219688 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 275 3 2 5 1.9 CN[C@@H]1CCN(c2cc(C3CCCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236576 219688 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 275 3 2 5 1.9 CN[C@@H]1CCN(c2cc(C3CCCCC3)nc(N)n2)C1 10.1021/jm401727m
1279 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
24745335 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
24745335 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None 6 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
53257796 219687 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236575 219687 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
24738269 140322 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.1 Nc1nc(N2CC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914543 140322 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.1 Nc1nc(N2CC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
1223 1963 35 None -21 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
44231735 22104 0 None -1 4 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089390 22104 0 None -1 4 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
44462956 19931 0 None 2 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL1077276 19931 0 None 2 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
1279 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1279 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 7960 58 None 3 7 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
137657169 315425 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 8 1 4 4.1 O=[N+]([O-])c1cccc(C(OCCCc2c[nH]cn2)c2ccccc2)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4102970 315425 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 337 8 1 4 4.1 O=[N+]([O-])c1cccc(C(OCCCc2c[nH]cn2)c2ccccc2)c1 10.1016/j.ejmech.2016.09.074
59777258 219673 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236561 219673 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
25130914 370502 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL492677 370502 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
46890547 20846 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
CHEMBL1082772 20846 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
10446295 4352 37 None 263 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
1277 4352 37 None 263 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
CHEMBL185951 4352 37 None 263 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
68081305 219662 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 1 1 2 1.3 CN1CCN(C(=O)c2cc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
CHEMBL3236550 219662 1 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 1 1 2 1.3 CN1CCN(C(=O)c2cc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
24798144 219665 0 None -18 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 219665 0 None -18 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
24738103 140401 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(OC)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914780 140401 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(OC)c23)C1 10.1016/j.bmcl.2011.08.014
24745335 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 607 14 None -8 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
16362 6358 55 None -81 22 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
2172 6358 55 None -81 22 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
90 6358 55 None -81 22 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
CHEMBL1423 6358 55 None -81 22 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
DB01100 6358 55 None -81 22 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
9904236 28317 25 None None None Human 5.7 pKi = 5.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 28317 25 None None None Human 5.7 pKi = 5.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
46890589 21351 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 7 1 4 4.8 Cc1cc(OCCCN2CCCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084809 21351 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 7 1 4 4.8 Cc1cc(OCCCN2CCCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57396382 140590 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 387 9 2 7 3.8 COCc1ccc(CN2CC[C@H](Nc3cc(NCCC(C)(C)C)ncn3)C2)o1 10.1016/j.bmcl.2011.07.114
CHEMBL1916495 140590 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 387 9 2 7 3.8 COCc1ccc(CN2CC[C@H](Nc3cc(NCCC(C)(C)C)ncn3)C2)o1 10.1016/j.bmcl.2011.07.114
57391122 140591 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 387 7 3 6 3.9 CC(C)(C)CCNc1cc(N[C@H]2CCN(Cc3cccc(F)c3O)C2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916496 140591 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 387 7 3 6 3.9 CC(C)(C)CCNc1cc(N[C@H]2CCN(Cc3cccc(F)c3O)C2)ncn1 10.1016/j.bmcl.2011.07.114
57394628 140596 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 4 2 5 1.7 CC(C)(C)CCNc1cc(N2CCNCC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916500 140596 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 4 2 5 1.7 CC(C)(C)CCNc1cc(N2CCNCC2)ncn1 10.1016/j.bmcl.2011.07.114
57397738 142110 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 245 1 0 5 0.1 CN1CCN(C(=O)c2cn3ccncc3n2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938841 142110 0 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 245 1 0 5 0.1 CN1CCN(C(=O)c2cn3ccncc3n2)CC1 10.1016/j.bmcl.2011.11.098
10399535 237242 2 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 2 2 1.6 CC1CN(C(=O)c2cc3ccccc3[nH]2)CCN1 10.1021/jm0341047
CHEMBL341087 237242 2 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 2 2 1.6 CC1CN(C(=O)c2cc3ccccc3[nH]2)CCN1 10.1021/jm0341047
90645147 221663 0 None 13 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
CHEMBL3290576 221663 0 None 13 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
90645147 221663 0 None 13 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290576 221663 0 None 13 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
155567108 350599 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 223 5 3 5 1.3 CC(C)(C)CNc1nccc(NCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597946 350599 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 223 5 3 5 1.3 CC(C)(C)CNc1nccc(NCCN)n1 10.1021/acs.jmedchem.9b01342
155536509 350439 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 274 6 3 5 2.3 CC(C)(C)CNc1nccc(NCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596582 350439 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 274 6 3 5 2.3 CC(C)(C)CNc1nccc(NCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
4687476 196659 4 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL261320 196659 4 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
9928073 468645 0 None -67 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm051008s
CHEMBL67284 468645 0 None -67 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm051008s
90654501 219845 0 None -21877 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238444 219845 0 None -21877 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
4687476 196659 4 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1021/jm7014217
CHEMBL261320 196659 4 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1021/jm7014217
10879463 19627 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106570 19627 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
46228132 465650 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL609161 465650 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
46228071 445819 12 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL596562 445819 12 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
51354870 121688 0 None -26 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 305 6 0 5 2.0 CN1CCN(CCCn2cc(CC3CCCCC3)nn2)CC1 10.1021/jm1013488
CHEMBL1688981 121688 0 None -26 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 305 6 0 5 2.0 CN1CCN(CCCn2cc(CC3CCCCC3)nn2)CC1 10.1021/jm1013488
57391928 142155 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4ccc(Cl)nc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938973 142155 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4ccc(Cl)nc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
135353317 427694 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 388 5 1 6 3.5 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5879056 427694 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 388 5 1 6 3.5 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
135353299 446126 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 288 4 1 4 3.9 CC(C)c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5968692 446126 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 288 4 1 4 3.9 CC(C)c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
23650960 295805 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(F)ccc2[nH]1 nan
CHEMBL3943309 295805 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(F)ccc2[nH]1 nan
42624149 219680 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3236568 219680 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1016/j.bmcl.2014.10.013
25218146 235962 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 2 0 4 2.6 CN1CCN(c2ccnc(-c3ccsc3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393521 235962 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 2 0 4 2.6 CN1CCN(c2ccnc(-c3ccsc3)c2)CC1 10.1016/j.bmcl.2014.12.027
42624149 219680 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 219680 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
53258370 219681 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236569 219681 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
57394548 140370 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@@H]3CCCN[C@@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914747 140370 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@@H]3CCCN[C@@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
57396298 140374 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 1 1 6 1.8 CN1CCN(c2nc(N)nc3c2oc2cccc(F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914752 140374 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 1 1 6 1.8 CN1CCN(c2nc(N)nc3c2oc2cccc(F)c23)CC1 10.1016/j.bmcl.2011.08.014
44628629 140389 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 269 1 2 6 1.4 Nc1nc(N2CCNCC2)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914767 140389 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 269 1 2 6 1.4 Nc1nc(N2CCNCC2)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
11630326 144784 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199231 144784 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
51354582 121682 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 6 1 4 3.3 CC(c1cn(CCCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
CHEMBL1688974 121682 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 6 1 4 3.3 CC(c1cn(CCCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
71603195 180552 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 283 3 2 5 1.9 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376798 180552 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 283 3 2 5 1.9 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
1251 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
3035842 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
CHEMBL18661 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
1530 4450 49 None -23442 24 Human 4.7 pKi = 4.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 4450 49 None -23442 24 Human 4.7 pKi = 4.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 4450 49 None -23442 24 Human 4.7 pKi = 4.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 4450 49 None -23442 24 Human 4.7 pKi = 4.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 4450 49 None -23442 24 Human 4.7 pKi = 4.7 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
57399107 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1021/acs.jmedchem.5b00516
CHEMBL1915532 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1021/acs.jmedchem.5b00516
57399107 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915532 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.125
57399107 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915532 140485 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.114
57395619 140486 9 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915533 140486 9 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.125
57395619 140486 9 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915533 140486 9 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
168268680 385309 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 385309 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
1403136 354383 7 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL475331 354383 7 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm800876b
1247 7944 80 None -199 11 Mouse 5.7 pKi = 5.7 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -199 11 Mouse 5.7 pKi = 5.7 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -199 11 Mouse 5.7 pKi = 5.7 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -199 11 Mouse 5.7 pKi = 5.7 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
164610824 368410 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856200 368410 0 None -14 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
10945113 212986 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL322256 212986 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
21896704 315366 0 None None None Human 6.7 pKi = 6.7 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 429 9 1 7 2.7 CC(=O)SCC(Cc1ccc2c(c1)OCO2)C(=O)NCC(=O)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4102243 315366 0 None None None Human 6.7 pKi = 6.7 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 429 9 1 7 2.7 CC(=O)SCC(Cc1ccc2c(c1)OCO2)C(=O)NCC(=O)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
46912441 25183 0 None -117 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172754 25183 0 None -117 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
118725538 235963 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 3 1 4 2.6 CN[C@@H]1CCN(c2ccnc(-c3ccsc3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393522 235963 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 3 1 4 2.6 CN[C@@H]1CCN(c2ccnc(-c3ccsc3)c2)C1 10.1016/j.bmcl.2014.12.027
1247 7944 80 None -12 11 Human 6.7 pKi = 6.7 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 6.7 pKi = 6.7 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 6.7 pKi = 6.7 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 6.7 pKi = 6.7 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
155567030 350385 0 None -645 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4596108 350385 0 None -645 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
24854708 311657 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 3 0 5 3.5 Cc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL405416 311657 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 3 0 5 3.5 Cc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
51354587 121687 0 None -3 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 0 5 2.7 c1cn(CCCn2cc(CC3CCCCC3)nn2)cn1 10.1021/jm1013488
CHEMBL1688979 121687 0 None -3 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 0 5 2.7 c1cn(CCCn2cc(CC3CCCCC3)nn2)cn1 10.1021/jm1013488
10702196 212956 1 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL320279 212956 1 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
136016345 24671 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 377 5 4 6 2.1 CCOC(=O)c1ccc(NC2=CC(=O)/C(=N\NC(=N)N)c3ccccc32)cc1 10.1021/jm7014777
CHEMBL1162352 24671 1 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 377 5 4 6 2.1 CCOC(=O)c1ccc(NC2=CC(=O)/C(=N\NC(=N)N)c3ccccc32)cc1 10.1021/jm7014777
135353300 410021 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 418 5 1 6 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncccn1)c1ccnc(N)n1 nan
CHEMBL5791975 410021 0 None None None Human 7.7 pKi = 7.7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 418 5 1 6 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncccn1)c1ccnc(N)n1 nan
127052293 277526 5 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1251 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
3035842 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
CHEMBL18661 4115 26 None -120 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
11258459 175204 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 412 6 1 4 4.5 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
CHEMBL220933 175204 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 412 6 1 4 4.5 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
46228082 465942 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 340 5 2 6 2.5 CC(C)c1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL610626 465942 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 340 5 2 6 2.5 CC(C)c1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
49841721 141972 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 347 2 1 5 3.2 Cc1cccc(C)c1-c1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
CHEMBL1935558 141972 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 347 2 1 5 3.2 Cc1cccc(C)c1-c1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
25178551 348289 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454882 348289 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm800876b
25178551 348289 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454882 348289 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm901379s
45379807 431640 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 438 6 1 6 3.5 CN1CCN(c2nc(NCCC(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591970 431640 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 438 6 1 6 3.5 CN1CCN(c2nc(NCCC(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10037650 19547 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 19547 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
122194624 252069 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1ccccc1/C=C/c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2015.08.014
CHEMBL3629827 252069 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1ccccc1/C=C/c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2015.08.014
57400700 140150 0 None -37 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910380 140150 0 None -37 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
164610421 368557 0 None -7 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4858567 368557 0 None -7 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
46890120 20867 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 416 6 1 4 5.2 Cc1cc(OCCCN2Cc3cccnc3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082851 20867 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 416 6 1 4 5.2 Cc1cc(OCCCN2Cc3cccnc3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
56851604 143857 0 None -13 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 398 8 2 3 5.1 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963460 143857 0 None -13 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 398 8 2 3 5.1 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
24853663 196387 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 272 3 0 5 1.8 CCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL259839 196387 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 272 3 0 5 1.8 CCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
24278976 196602 47 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 1 0 4 2.0 CN1CCN(c2nc3ccccc3nc2Cl)CC1 10.1021/jm7014217
CHEMBL261010 196602 47 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 1 0 4 2.0 CN1CCN(c2nc3ccccc3nc2Cl)CC1 10.1021/jm7014217
24854704 196488 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2ccc(Cl)cc2)CC1 10.1021/jm7014217
CHEMBL260456 196488 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2ccc(Cl)cc2)CC1 10.1021/jm7014217
10923241 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128958 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
137395043 405765 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 349 4 1 6 3.7 Cc1cc(C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5748712 405765 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 349 4 1 6 3.7 Cc1cc(C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353308 462330 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 362 7 1 6 3.2 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1CC(C)C nan
CHEMBL6038774 462330 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 362 7 1 6 3.2 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1CC(C)C nan
10923241 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128958 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0341047
56835171 141988 0 None -1 9 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from mouse H4RDisplacement of [3H]histamine from mouse H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 141988 0 None -1 9 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from mouse H4RDisplacement of [3H]histamine from mouse H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
11687917 38863 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
CHEMBL120854 38863 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
10923241 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128958 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
45257131 444119 0 None 18 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 444119 0 None 18 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
57403350 140593 0 None 35 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 3 1 5 1.7 CN1CCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916498 140593 0 None 35 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 3 1 5 1.7 CN1CCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
58227385 404908 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 247 5 2 5 1.1 CN[C@@H]1CCN(c2cnnc(NCC3CC3)c2)C1 nan
CHEMBL5740458 404908 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 247 5 2 5 1.1 CN[C@@H]1CCN(c2cnnc(NCC3CC3)c2)C1 nan
24804058 290856 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 424 7 2 5 5.1 Cc1c(F)ccc2[nH]c(-c3cnc(NCCCC4CCN(C)CC4)nc3C(C)C)nc12 nan
CHEMBL3903520 290856 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 424 7 2 5 5.1 Cc1c(F)ccc2[nH]c(-c3cnc(NCCCC4CCN(C)CC4)nc3C(C)C)nc12 nan
126963284 291521 0 None None None Human 5.6 pKi = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL3909134 291521 0 None None None Human 5.6 pKi = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
46890675 21562 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 1 4 4.4 Cc1cc(OCCCN2CC3CCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1085803 21562 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 1 4 4.4 Cc1cc(OCCCN2CC3CCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
49841722 141973 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3c(-c4ccc(C#N)cc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935559 141973 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3c(-c4ccc(C#N)cc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
168276867 385378 0 None -6 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 385378 0 None -6 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
24853598 196575 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 350 4 0 6 3.2 COc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL260851 196575 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 350 4 0 6 3.2 COc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
24853596 196646 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 354 3 0 5 3.8 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)cc2)CC1 10.1021/jm7014217
CHEMBL261225 196646 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 354 3 0 5 3.8 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)cc2)CC1 10.1021/jm7014217
164610289 368433 0 None -38 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856602 368433 0 None -38 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
57399827 140597 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916501 140597 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
90645155 221669 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290582 221669 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
90645155 221669 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL3290582 221669 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
46228114 445812 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596551 445812 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25178131 370195 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 381 5 1 5 3.7 CN1CCN(c2nc(NCCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL490072 370195 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 381 5 1 5 3.7 CN1CCN(c2nc(NCCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
90645152 221666 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 396 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(I)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290579 221666 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 396 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(I)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
135353331 412864 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 362 6 2 6 3.3 CCOc1cc(F)ccc1N(Cc1n[nH]cc1Cl)c1ccnc(N)n1 nan
CHEMBL5823541 412864 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 362 6 2 6 3.3 CCOc1cc(F)ccc1N(Cc1n[nH]cc1Cl)c1ccnc(N)n1 nan
135353367 444311 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5949088 444311 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353327 445368 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ccon1)c1ccnc(N)n1 nan
CHEMBL5960609 445368 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ccon1)c1ccnc(N)n1 nan
49818718 141978 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935564 141978 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
54582867 124317 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770999 124317 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
58227165 235977 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 nan
CHEMBL3393536 235977 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 nan
25147771 348296 0 None 1 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 348296 0 None 1 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
11440060 473958 0 None None None Human 6.6 pKi = 6.6 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 368 8 1 2 5.4 c1ccc(C(OCCCc2c[nH]cn2)(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL91576 473958 0 None None None Human 6.6 pKi = 6.6 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 368 8 1 2 5.4 c1ccc(C(OCCCc2c[nH]cn2)(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
58227114 464773 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 273 3 2 5 1.5 c1cc(N2CCNCC2)nc(NC2CC3CCC2C3)n1 nan
CHEMBL6063758 464773 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 273 3 2 5 1.5 c1cc(N2CCNCC2)nc(NC2CC3CCC2C3)n1 nan
127051301 277488 0 None 5 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None 5 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227216 235995 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393554 235995 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
550981 141295 9 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
CHEMBL1923533 141295 9 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
24804056 297309 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 420 8 2 5 5.1 CCCc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(C)ccc2[nH]1 nan
CHEMBL3955597 297309 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 420 8 2 5 5.1 CCCc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(C)ccc2[nH]1 nan
135353379 414177 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 373 6 1 8 2.4 CCc1cc(S(C)(=O)=O)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5837439 414177 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 373 6 1 8 2.4 CCc1cc(S(C)(=O)=O)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
71461658 160547 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 259 1 2 4 0.5 CN1CCN(C(=O)c2nc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL2113162 160547 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 259 1 2 4 0.5 CN1CCN(C(=O)c2nc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
4024 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
9989505 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
CHEMBL82298 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
122193101 251974 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.4 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C(F)(F)F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628048 251974 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.4 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C(F)(F)F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
155546701 347743 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 264 2 1 6 0.8 CN1CCN(c2nc(N)nc(CC(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4534504 347743 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 264 2 1 6 0.8 CN1CCN(c2nc(N)nc(CC(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
24798596 443897 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594491 443897 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
137395072 430394 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 330 6 1 8 2.3 CCOc1cc(F)ccc1N(Cc1nnco1)c1ccnc(N)n1 nan
CHEMBL5906972 430394 0 None None None Human 6.6 pKi = 6.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 330 6 1 8 2.3 CCOc1cc(F)ccc1N(Cc1nnco1)c1ccnc(N)n1 nan
21193534 25544 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 292 7 1 2 4.1 c1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL1179089 25544 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 292 7 1 2 4.1 c1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
135353335 431768 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 372 6 1 6 3.4 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C2CC2)cc1C1CCC1 nan
CHEMBL5921061 431768 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 372 6 1 6 3.4 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C2CC2)cc1C1CCC1 nan
54587789 124294 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(NCCO)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770976 124294 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(NCCO)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
45257131 444119 0 None 18 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 444119 0 None 18 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
90655027 219667 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236555 219667 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
66740898 219674 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
CHEMBL3236562 219674 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
24826082 140412 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914791 140412 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
11587279 253067 3 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
CHEMBL364400 253067 3 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
1226 4125 18 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 4125 18 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 4125 18 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
10105117 213914 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 213914 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10466840 469383 0 None 398 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72424 469383 0 None 398 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
71681476 180485 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 316 8 4 8 1.5 CC(C)CCc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375756 180485 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 316 8 4 8 1.5 CC(C)CCc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
4060730 43234 34 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm301886t
CHEMBL129199 43234 34 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm301886t
10923241 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL128958 43019 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
4060730 43234 34 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129199 43234 34 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
22660616 157312 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3ccc(O)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047273 157312 1 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3ccc(O)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
71525588 180559 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.1 CNC1CN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376805 180559 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.1 CNC1CN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846300 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm7014217
CHEMBL213912 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm7014217
45271470 389595 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 288 6 3 3 3.1 Cc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL549481 389595 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 288 6 3 3 3.1 Cc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
45270644 390314 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 257 6 4 2 1.7 N=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmc.2009.04.007
CHEMBL552694 390314 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 257 6 4 2 1.7 N=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmc.2009.04.007
45271464 390408 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 292 6 3 3 2.9 N=C(NCc1ccc(F)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL553455 390408 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 292 6 3 3 2.9 N=C(NCc1ccc(F)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10468601 390593 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL555434 390593 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45268095 392580 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 378 9 3 3 4.8 N=C(NCCC(c1ccccc1)c1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560313 392580 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 378 9 3 3 4.8 N=C(NCCC(c1ccccc1)c1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1247 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 7944 80 None -12 11 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1274 8815 10 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
3063228 8815 10 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
CHEMBL1196470 8815 10 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
10988959 236934 2 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL340740 236934 2 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1039/C2MD20212C
44546968 449829 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 232 4 2 4 1.3 c1cc(N2CCNCC2)cc(NCC2CC2)n1 nan
CHEMBL6008473 449829 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 232 4 2 4 1.3 c1cc(N2CCNCC2)cc(NCC2CC2)n1 nan
21638785 371849 3 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 371849 3 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127052294 277590 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 277590 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11751419 275269 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
CHEMBL376268 275269 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
11751419 275269 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2006.08.117
CHEMBL376268 275269 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2006.08.117
57402512 140438 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915022 140438 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
46228092 444377 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 299 4 1 6 1.4 CN1CCN(c2cc(OCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594973 444377 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 299 4 1 6 1.4 CN1CCN(c2cc(OCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
4024 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 4117 17 None -301 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
1252 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
9793868 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL417096 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1237 7956 17 None -676 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 7956 17 None -676 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 7956 17 None -676 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1252 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
9793868 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL417096 4121 15 None -79 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
81371 27035 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 178 3 4 4 0.2 N=C(N)SCCSC(=N)N 10.1021/jm060880d
CHEMBL1187946 27035 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 178 3 4 4 0.2 N=C(N)SCCSC(=N)N 10.1021/jm060880d
52128564 157298 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 278 1 0 3 2.5 CN1CCN(C(=O)c2cc3cc(Cl)ccc3o2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047259 157298 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 278 1 0 3 2.5 CN1CCN(C(=O)c2cc3cc(Cl)ccc3o2)CC1 10.1016/j.ejmech.2012.06.016
70684084 157334 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 2 2 2.6 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047452 157334 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 2 2 2.6 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
70692528 157340 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047458 157340 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70686224 157354 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 2 2 2 2.4 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047472 157354 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 2 2 2 2.4 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
51355156 121694 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 3.1 c1nc(CCCc2cn(C3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688989 121694 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 3.1 c1nc(CCCc2cn(C3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
9990475 119277 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
CHEMBL1632408 119277 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
10583206 212980 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321920 212980 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
71681640 180492 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 356 6 4 8 2.3 Nc1nc(Cl)cc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375763 180492 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 356 6 4 8 2.3 Nc1nc(Cl)cc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
12438303 157297 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 260 1 0 3 2.3 CN1CCN(C(=O)c2cc3ccccc3s2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047258 157297 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 260 1 0 3 2.3 CN1CCN(C(=O)c2cc3ccccc3s2)CC1 10.1016/j.ejmech.2012.06.016
22660598 157322 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047440 157322 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24854636 312240 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 296 1 0 4 2.4 CN1CCN(c2nc3ccccc3nc2C(F)(F)F)CC1 10.1021/jm7014217
CHEMBL406558 312240 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 296 1 0 4 2.4 CN1CCN(c2nc3ccccc3nc2C(F)(F)F)CC1 10.1021/jm7014217
10583206 212980 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321920 212980 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
44395263 138991 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 292 2 2 3 1.7 CN1CCN(NC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL185546 138991 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 292 2 2 3 1.7 CN1CCN(NC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
44395336 139077 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 280 4 1 3 1.9 CN(C)CCN(C)C(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL185948 139077 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 280 4 1 3 1.9 CN(C)CCN(C)C(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
44395290 253517 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 279 4 1 2 2.5 CN(C)CCN(C)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL364629 253517 0 None None None Human 4.6 pKi = 4.6 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 279 4 1 2 2.5 CN(C)CCN(C)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
15984057 277412 0 None -35481 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 348 5 0 2 5.3 c1cc(-c2ccc(CN3CCCCC3)cc2)ccc1CN1CCCCC1 10.1016/j.bmc.2008.10.029
CHEMBL380101 277412 0 None -35481 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 348 5 0 2 5.3 c1cc(-c2ccc(CN3CCCCC3)cc2)ccc1CN1CCCCC1 10.1016/j.bmc.2008.10.029
71519348 177367 0 None None None Human 4.6 pKi = 4.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 308 3 2 6 1.5 Nc1nc(N2CCNCC2)c2ccn(Cc3ccccc3)c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314766 177367 0 None None None Human 4.6 pKi = 4.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 308 3 2 6 1.5 Nc1nc(N2CCNCC2)c2ccn(Cc3ccccc3)c2n1 10.1016/j.bmcl.2012.10.139
122193106 251978 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 335 3 2 6 1.9 CN1CCN(c2nc(N)nc(/C=C/c3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628052 251978 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 335 3 2 6 1.9 CN1CCN(c2nc(N)nc(/C=C/c3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
122193095 251968 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628042 251968 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
54585776 124279 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(N)nc(NCCO)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770961 124279 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(N)nc(NCCO)n2)C1 10.1016/j.bmcl.2011.03.017
24994630 219671 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 2 5 1.6 Nc1nc(C2CCCC2)cc(N2CCC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236559 219671 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 2 5 1.6 Nc1nc(C2CCCC2)cc(N2CCC[C@@H](N)C2)n1 10.1021/jm401727m
25178933 370194 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL490071 370194 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178933 370194 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL490071 370194 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
122193103 251976 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 341 4 1 8 1.3 CN1CCN(c2nc(N)nc(/C=C/c3cccc([N+](=O)[O-])c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628050 251976 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 341 4 1 8 1.3 CN1CCN(c2nc(N)nc(/C=C/c3cccc([N+](=O)[O-])c3)n2)CC1 10.1016/j.ejmech.2015.08.014
135353287 430587 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 356 6 1 6 2.8 CCc1cc(S(=O)(=O)C(F)F)ccc1N(CC)c1ccnc(N)n1 nan
CHEMBL5908930 430587 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 356 6 1 6 2.8 CCc1cc(S(=O)(=O)C(F)F)ccc1N(CC)c1ccnc(N)n1 nan
135353483 464945 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 354 4 1 4 5.2 CCN(c1ccnc(N)n1)c1ccc(S(F)(F)(F)(F)F)cc1C nan
CHEMBL6065537 464945 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 354 4 1 4 5.2 CCN(c1ccnc(N)n1)c1ccc(S(F)(F)(F)(F)F)cc1C nan
10446295 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
1277 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL185951 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
10446295 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
1277 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
CHEMBL185951 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
46890627 20919 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083098 20919 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
11340020 175235 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
CHEMBL221210 175235 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
136042265 142156 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938974 142156 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
11340020 175235 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL221210 175235 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
11189343 279156 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 420 6 1 4 4.9 Cc1cc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)ccc1OCCCN1CCN(C)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL387342 279156 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 420 6 1 4 4.9 Cc1cc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)ccc1OCCCN1CCN(C)CC1 10.1016/j.bmcl.2006.08.117
57394549 140371 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914748 140371 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
10446295 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
58227306 432100 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 221 4 2 5 0.7 CC(C)CNc1nccc(N2CC(N)C2)n1 nan
CHEMBL5924522 432100 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 221 4 2 5 0.7 CC(C)CNc1nccc(N2CC(N)C2)n1 nan
24759624 196486 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 0 5 2.0 COc1nc2cc(Cl)ccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL260444 196486 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 0 5 2.0 COc1nc2cc(Cl)ccc2nc1N1CCN(C)CC1 10.1021/jm7014217
25147771 348296 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 348296 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
44129211 450851 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 383 5 1 7 1.5 CN1CCN(c2nc(NCCS(C)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL601946 450851 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 383 5 1 7 1.5 CN1CCN(c2nc(NCCS(C)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11821243 42711 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 2 1 2 1.9 CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128134 42711 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 2 1 2 1.9 CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
155549319 350293 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 5 2 5 2.0 CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595399 350293 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 5 2 5 2.0 CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
164620704 369363 0 None -17 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 369363 0 None -17 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
127026016 274892 0 None -13 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753967 274892 0 None -13 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
71518861 177374 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 326 2 2 5 2.1 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314774 177374 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 326 2 2 5 2.1 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
122193102 251975 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 321 3 1 7 1.2 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628049 251975 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 321 3 1 7 1.2 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
63868018 349379 1 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 208 1 1 6 -0.5 Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4574940 349379 1 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 208 1 1 6 -0.5 Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71518536 177371 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 232 1 3 5 0.3 Cc1cc2c(N3CCNCC3)nc(N)nc2[nH]1 10.1016/j.bmcl.2012.10.139
CHEMBL2314771 177371 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 232 1 3 5 0.3 Cc1cc2c(N3CCNCC3)nc(N)nc2[nH]1 10.1016/j.bmcl.2012.10.139
57391927 142150 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938969 142150 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
3991311 274285 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 296 2 0 5 2.7 CCc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
CHEMBL3741986 274285 7 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 296 2 0 5 2.7 CCc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
25178556 372243 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL509961 372243 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
44563707 466143 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccc(Cl)cc3nc2OCc2ccccc2)CC1 10.1021/jm800876b
CHEMBL612059 466143 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccc(Cl)cc3nc2OCc2ccccc2)CC1 10.1021/jm800876b
24853595 315924 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2cccc(Cl)c2)CC1 10.1021/jm7014217
CHEMBL410925 315924 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2cccc(Cl)c2)CC1 10.1021/jm7014217
155535098 350355 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 3 3 5 1.3 CC(C)(C)CNc1nccc(N2CCCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595908 350355 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 3 3 5 1.3 CC(C)(C)CNc1nccc(N2CCCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
10782821 196574 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 332 4 0 4 3.4 CCN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260850 196574 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 332 4 0 4 3.4 CCN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
164616851 368254 0 None -446 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 368254 0 None -446 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
10591811 315198 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 9 1 2 4.7 c1ccc(-c2ccc(CCCOCCCc3c[nH]cn3)cc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4100315 315198 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 9 1 2 4.7 c1ccc(-c2ccc(CCCOCCCc3c[nH]cn3)cc2)cc1 10.1016/j.ejmech.2016.09.074
135353309 432327 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cnco1)c1ccnc(N)n1 nan
CHEMBL5926588 432327 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cnco1)c1ccnc(N)n1 nan
10446295 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.ejmech.2023.115151
1277 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.ejmech.2023.115151
CHEMBL185951 4352 37 None 263 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.ejmech.2023.115151
1267 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
3035905 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
CHEMBL260374 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
24804219 295245 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 378 6 2 5 4.2 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cccc2[nH]1 nan
CHEMBL3938862 295245 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 378 6 2 5 4.2 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cccc2[nH]1 nan
11565330 197533 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
CHEMBL268525 197533 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
1267 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
3035905 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
CHEMBL260374 8287 36 None -28 9 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
71525681 180557 0 None -4 6 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 180557 0 None -4 6 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846634 159587 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209758 159587 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
57395496 140444 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915034 140444 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
51354302 121678 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688970 121678 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25130235 370821 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 370821 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 370821 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 370821 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
57390225 140154 0 None -60 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910384 140154 0 None -60 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
55251397 347366 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 236 2 1 6 0.3 CC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4525008 347366 1 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 236 2 1 6 0.3 CC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
135350650 410004 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 341 5 1 6 4.1 C/C=C/c1cc(Cl)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5791863 410004 0 None None None Human 7.6 pKi = 7.6 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 341 5 1 6 4.1 C/C=C/c1cc(Cl)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
53233803 124280 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770962 124280 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
11293460 175799 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 434 6 1 4 5.1 CN1CCN(CCCOc2ccc(-c3nc4c(ccc5ccccc54)[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL223490 175799 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 434 6 1 4 5.1 CN1CCN(CCCOc2ccc(-c3nc4c(ccc5ccccc54)[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
42624148 219686 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236574 219686 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
11846300 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
CHEMBL213912 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
11846300 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 161722 3 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
217674 353174 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL473098 353174 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
217674 353174 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL473098 353174 2 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
156009715 352235 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 601 8 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/c3cc4c5c(c3)CCCN5CCC4)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4651103 352235 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 601 8 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/c3cc4c5c(c3)CCCN5CCC4)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
45257134 444353 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
CHEMBL594949 444353 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
155539562 346968 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 304 4 1 6 1.7 CN1CCN(c2nc(N)nc(CCC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4514667 346968 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 304 4 1 6 1.7 CN1CCN(c2nc(N)nc(CCC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
10083188 278200 2 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL382276 278200 2 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
9927983 161314 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 341 1 0 4 4.2 CCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL212212 161314 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 341 1 0 4 4.2 CCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
135353362 432913 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 345 6 1 7 3.4 CCOc1cc(F)ccc1N(Cc1cscn1)c1ccnc(N)n1 nan
CHEMBL5932310 432913 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 345 6 1 7 3.4 CCOc1cc(F)ccc1N(Cc1cscn1)c1ccnc(N)n1 nan
135353341 443957 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 427 6 1 8 3.2 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5945466 443957 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 427 6 1 8 3.2 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353369 445035 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 365 5 1 7 3.6 Cc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5956987 445035 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 365 5 1 7 3.6 Cc1cc(OC(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
49841612 141982 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3cc(-c4ccc(C#N)cc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935568 141982 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3cc(-c4ccc(C#N)cc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
54587786 124288 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770970 124288 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
24825897 140381 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 1 1 6 2.2 CN1CCN(c2nc(N)nc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914759 140381 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 1 1 6 2.2 CN1CCN(c2nc(N)nc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
71519674 180558 0 None -5 5 Rat 7.5 pKi = 7.5 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 180558 0 None -5 5 Rat 7.5 pKi = 7.5 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
56851610 143855 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 5 2 3 3.8 CC(C)(C)N/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963448 143855 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 5 2 3 3.8 CC(C)(C)N/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
127049856 277533 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805431 277533 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
10680721 20311 0 None -23 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 225 6 2 3 1.9 CC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1080089 20311 0 None -23 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 225 6 2 3 1.9 CC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
753256 353242 8 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL473662 353242 8 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46228133 444980 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595639 444980 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
29136870 141285 6 None -46 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
CHEMBL1923522 141285 6 None -46 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
71519176 177360 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 2 2 5 2.5 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314759 177360 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 2 2 5 2.5 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
137394991 425420 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 2 7 2.1 CCOc1cc(F)ccc1N(Cc1cn[nH]n1)c1ccnc(N)n1 nan
CHEMBL5853597 425420 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 2 7 2.1 CCOc1cc(F)ccc1N(Cc1cn[nH]n1)c1ccnc(N)n1 nan
155545717 347566 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 238 3 2 2 2.6 c1ccc2[nH]c(C[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
CHEMBL4529871 347566 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 238 3 2 2 2.6 c1ccc2[nH]c(C[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
156015791 352159 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 442 8 1 3 4.6 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCN1CCc2nc[nH]c2C1 10.1021/acs.jmedchem.0c00160
CHEMBL4650609 352159 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 442 8 1 3 4.6 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCN1CCc2nc[nH]c2C1 10.1021/acs.jmedchem.0c00160
24854638 311184 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL402470 311184 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCc2ccccc2)CC1 10.1021/jm7014217
24854702 196412 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2cccnc2)CC1 10.1021/jm7014217
CHEMBL259955 196412 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2cccnc2)CC1 10.1021/jm7014217
24853592 312081 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 376 7 0 5 3.8 CN1CCN(c2nc3ccccc3nc2OCCCCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL406380 312081 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 376 7 0 5 3.8 CN1CCN(c2nc3ccccc3nc2OCCCCc2ccccc2)CC1 10.1021/jm7014217
122193104 251943 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3627724 251943 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
137632569 312196 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 418 7 1 2 4.8 Ic1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4065099 312196 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 418 7 1 2 4.8 Ic1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
135353302 433313 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 364 5 1 5 4.2 CC(C)Oc1cc(Br)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5936665 433313 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 364 5 1 5 4.2 CC(C)Oc1cc(Br)ccc1N(c1ccnc(N)n1)C(C)C nan
53233804 124284 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770966 124284 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
54583873 124287 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770969 124287 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
54584824 124295 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770977 124295 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
54585780 124316 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770998 124316 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
58227326 235983 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393542 235983 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
9839217 144732 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199062 144732 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
58227255 235980 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 nan
CHEMBL3393539 235980 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 nan
54583873 124287 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL1770969 124287 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
54585781 124319 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
CHEMBL1771000 124319 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
71551636 180502 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 263 4 1 5 1.4 CC(C)CCc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
CHEMBL2375772 180502 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 263 4 1 5 1.4 CC(C)CCc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
25129527 370651 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm301886t
CHEMBL493720 370651 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm301886t
46881855 22065 0 None 15 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089040 22065 0 None 15 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
10967174 43294 1 None 3 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 43294 1 None 3 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
46890166 21636 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 21636 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1279 7960 58 None -3 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -3 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -3 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
71603136 180544 0 None 46 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 3 2 5 2.3 CNC1CN(c2nc(N)nc3cc(C4CCCC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376790 180544 0 None 46 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 3 2 5 2.3 CNC1CN(c2nc(N)nc3cc(C4CCCC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
25109291 366002 9 None -79 12 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 366002 9 None -79 12 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
127050309 270584 0 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 283 2 2 6 1.8 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1039/C6MD00108D
CHEMBL3819470 270584 0 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 283 2 2 6 1.8 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1039/C6MD00108D
53476465 140326 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 2 2 6 2.0 NCC1CN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914547 140326 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 2 2 6 2.0 NCC1CN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24737947 140398 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 283 2 2 6 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914776 140398 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 283 2 2 6 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1016/j.bmcl.2011.08.014
25071004 385261 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 385261 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
44547124 430884 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 4 2 4 1.7 CC(C)CNc1cc(N2CC[C@@H](N)C2)ccn1 nan
CHEMBL5912000 430884 0 None None None Human 8.5 pKi = 8.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 4 2 4 1.7 CC(C)CNc1cc(N2CC[C@@H](N)C2)ccn1 nan
25071004 385261 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 385261 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
11957573 4107 26 None -7 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
1250 4107 26 None -7 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
3692 4107 26 None -7 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL19439 4107 26 None -7 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
24826358 140368 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 1 2 6 2.4 Nc1nc(N2CC3CCNC3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914745 140368 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 1 2 6 2.4 Nc1nc(N2CC3CCNC3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25101945 385646 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 385646 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
58227401 350418 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 350418 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
25068753 371642 21 None 1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 371642 21 None 1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1279 7960 58 None -4 7 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -4 7 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -4 7 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1267 8287 36 None -28 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 8287 36 None -28 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 8287 36 None -28 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
21638785 371849 3 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 371849 3 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
135353350 408613 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 415 6 1 6 3.7 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)N2CCCC2)cc1C1CCC1 nan
CHEMBL5777304 408613 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 415 6 1 6 3.7 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)N2CCCC2)cc1C1CCC1 nan
135353323 412923 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 3 1 4 4.4 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1C(F)(F)F nan
CHEMBL5824203 412923 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 3 1 4 4.4 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1C(F)(F)F nan
135353312 425330 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 388 6 1 6 4.1 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(C)C)cc1C1CCC1 nan
CHEMBL5852660 425330 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 388 6 1 6 4.1 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(C)C)cc1C1CCC1 nan
135350853 425610 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 326 4 1 5 3.8 Cc1cc(OC(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5855845 425610 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 326 4 1 5 3.8 Cc1cc(OC(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
24994636 219677 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
CHEMBL3236565 219677 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
24826441 140376 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1cccc2oc3c(N4CCN(C)CC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
CHEMBL1914754 140376 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1cccc2oc3c(N4CCN(C)CC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
10244243 278547 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL383384 278547 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
73353369 180542 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 6 0.4 CN1CCN(c2nc(N)nc3cccnc23)CC1 10.1016/j.bmcl.2013.02.091
CHEMBL2376788 180542 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 6 0.4 CN1CCN(c2nc(N)nc3cccnc23)CC1 10.1016/j.bmcl.2013.02.091
11846636 159535 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209628 159535 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
155513612 350289 0 None -4 4 Mouse 7.5 pKi = 7.5 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 350289 0 None -4 4 Mouse 7.5 pKi = 7.5 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
206876 42802 4 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL128637 42802 4 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
206876 42802 4 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128637 42802 4 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
11249610 313852 0 None -6309 2 Human 4.5 pKi = 4.5 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 354 9 2 5 3.6 Nc1ccc(NCCc2ccc(OCCCN3CCCCC3)cc2)nc1 10.1016/j.ejmech.2016.09.074
CHEMBL4084820 313852 0 None -6309 2 Human 4.5 pKi = 4.5 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 354 9 2 5 3.6 Nc1ccc(NCCc2ccc(OCCCN3CCCCC3)cc2)nc1 10.1016/j.ejmech.2016.09.074
137634777 311903 0 None None None Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 453 8 3 6 1.0 CCOC(=O)CN1Cc2ccccc2C[C@@H](NC(=O)C(Cc2ccccc2)C(=O)NO)C1=O 10.1016/j.ejmech.2016.09.074
CHEMBL4061504 311903 0 None None None Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 453 8 3 6 1.0 CCOC(=O)CN1Cc2ccccc2C[C@@H](NC(=O)C(Cc2ccccc2)C(=O)NO)C1=O 10.1016/j.ejmech.2016.09.074
164611474 368741 0 None -478 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
CHEMBL4861704 368741 0 None -478 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
164619427 369349 0 None -7 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4871221 369349 0 None -7 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
164627774 369831 0 None -58 6 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 369831 0 None -58 6 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
24994634 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
24994634 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
8984 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL3236549 4374 36 None -58 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
155552341 350353 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 4 3 5 1.7 CC(C)(C)CNc1nccc(NC2CCNC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595906 350353 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 4 3 5 1.7 CC(C)(C)CNc1nccc(NC2CCNC2)n1 10.1021/acs.jmedchem.9b01342
44129283 451223 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3ccc(Cl)c(Cl)c3n2)CC1 10.1021/jm901379s
CHEMBL602330 451223 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3ccc(Cl)c(Cl)c3n2)CC1 10.1021/jm901379s
11846299 276546 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
CHEMBL378788 276546 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
10934567 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
CHEMBL129026 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
137395041 411152 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 328 6 2 6 2.7 CCOc1cc(F)ccc1N(Cc1cc[nH]n1)c1ccnc(N)n1 nan
CHEMBL5804462 411152 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 328 6 2 6 2.7 CCOc1cc(F)ccc1N(Cc1cc[nH]n1)c1ccnc(N)n1 nan
135350867 446155 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 417 9 1 6 3.9 CCCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)N(C)CCC)cc1C1CCC1 nan
CHEMBL5969048 446155 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 417 9 1 6 3.9 CCCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)N(C)CCC)cc1C1CCC1 nan
135350541 449415 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 461 6 2 7 4.3 CCc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6004368 449415 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 461 6 2 7 4.3 CCc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
58227362 464396 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 6 2 5 1.5 CCCCNc1cc(N2CC[C@@H](NC)C2)cnn1 nan
CHEMBL6059511 464396 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 6 2 5 1.5 CCCCNc1cc(N2CC[C@@H](NC)C2)cnn1 nan
10934567 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL129026 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
25128833 371611 26 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL501882 371611 26 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1016/j.bmcl.2011.10.104
24826354 140411 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914790 140411 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
10934567 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL129026 43114 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
16006947 270538 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL378619 270538 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
58227260 235987 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 nan
CHEMBL3393546 235987 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 nan
136030655 119281 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
9923162 42797 10 None 199 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL128613 42797 10 None 199 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
170389 473913 24 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL91353 473913 24 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1274 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
170389 473913 24 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 473913 24 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681808 180477 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 392 9 3 8 3.1 CC(C)CNc1nccc(NCCN(C)c2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375748 180477 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 392 9 3 8 3.1 CC(C)CNc1nccc(NCCN(C)c2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
1274 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
3063228 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
CHEMBL1196470 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
56851608 143858 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 334 6 2 3 4.3 c1nc(CCCS/C(=N\C2CCCC2)NC2CCCCC2)c[nH]1 10.1021/jm201042n
CHEMBL1963461 143858 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 334 6 2 3 4.3 c1nc(CCCS/C(=N\C2CCCC2)NC2CCCCC2)c[nH]1 10.1021/jm201042n
1274 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
3063228 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
CHEMBL1196470 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
1279 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
66572105 157302 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047263 157302 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572106 157303 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3c(Cl)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047264 157303 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3c(Cl)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573463 157336 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 2 3.1 Cc1cc(Cl)cc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047454 157336 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 317 2 1 2 3.1 Cc1cc(Cl)cc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
70696622 157351 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047469 157351 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10988959 236934 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL340740 236934 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10087533 392550 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 322 7 3 3 3.5 N=C(NCCc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560068 392550 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 322 7 3 3 3.5 N=C(NCCc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
46929648 40643 0 None -6 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243395 40643 0 None -6 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
137650793 313342 0 None -1096 2 Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 484 7 1 4 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc(Br)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4078910 313342 0 None -1096 2 Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 484 7 1 4 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc(Br)c1 10.1016/j.ejmech.2016.09.074
46912442 25185 0 None -575 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172775 25185 0 None -575 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
57392460 142112 0 None 14 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938843 142112 0 None 14 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.bmcl.2011.11.098
136192886 119279 0 None -6 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632411 119279 0 None -6 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1248 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
1240 4168 15 None -125 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 4168 15 None -125 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 4168 15 None -125 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
71681976 180480 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 5 4 5 2.0 Nc1nccc(NCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)n1 10.1021/jm301886t
CHEMBL2375751 180480 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 5 4 5 2.0 Nc1nccc(NCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)n1 10.1021/jm301886t
10023327 333639 0 None -144 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11622672 156687 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203389 156687 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
11679919 157207 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204413 157207 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCNCCCCCc1c[nH]cn1 10.1021/jm0504353
11701199 157238 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 1 2 2.1 CCN(CC)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204615 157238 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 1 2 2.1 CCN(CC)CCCCc1c[nH]cn1 10.1021/jm0504353
1248 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
3077 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
90045 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
CHEMBL12344 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
4060730 43234 34 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 43234 34 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
10377814 157307 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3c(N)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047268 157307 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3c(N)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1248 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
3077 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
90045 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
CHEMBL12344 2933 20 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
4563101 139045 7 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 265 4 2 2 2.1 CN(C)CCNC(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL185842 139045 7 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 265 4 2 2 2.1 CN(C)CCNC(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
71681977 180481 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 344 5 3 5 2.4 CN(CCNc1ccnc(N)n1)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm301886t
CHEMBL2375752 180481 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 344 5 3 5 2.4 CN(CCNc1ccnc(N)n1)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm301886t
71681479 180489 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 393 9 5 9 2.7 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375760 180489 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 393 9 5 9 2.7 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
3063453 27037 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 189 5 5 3 -0.1 N=C(N)NCCCCSC(=N)N 10.1021/jm060880d
CHEMBL1187950 27037 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 189 5 5 3 -0.1 N=C(N)NCCCCSC(=N)N 10.1021/jm060880d
112936341 274877 0 None -12 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753849 274877 0 None -12 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
164628701 369735 0 None -186 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 369735 0 None -186 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
57402928 142111 0 None 9 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 278 1 0 4 1.4 CN1CCN(C(=O)c2cn3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938842 142111 0 None 9 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 278 1 0 4 1.4 CN1CCN(C(=O)c2cn3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.11.098
121238071 332032 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 271 2 1 7 0.3 CN1CCN(c2nc(N)nc(-c3ccncc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4292486 332032 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 271 2 1 7 0.3 CN1CCN(c2nc(N)nc(-c3ccncc3)n2)CC1 10.1016/j.ejmech.2017.09.035
11120826 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128505 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1007/s00044-004-0106-7
135353319 412260 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 386 7 1 6 3.8 CCCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C2CC2)cc1C1CCC1 nan
CHEMBL5816616 412260 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 386 7 1 6 3.8 CCCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C2CC2)cc1C1CCC1 nan
135353310 448836 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 6 1 6 3.3 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
CHEMBL5998028 448836 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 6 1 6 3.3 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
11120826 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128505 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0341047
49841720 141971 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3c(-c4ccccc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935557 141971 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3c(-c4ccccc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
44275465 199440 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL281590 199440 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
46890545 21705 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 6 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086460 21705 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 6 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
11120826 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128505 42777 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
57399829 140601 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 235 7 2 5 1.3 CN(C)CCNc1cc(NCC2CC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916505 140601 1 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 235 7 2 5 1.3 CN(C)CCNc1cc(NCC2CC2)ncn1 10.1016/j.bmcl.2011.07.114
44126357 234850 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(N)nc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354813 234850 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(N)nc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
57393772 140448 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Br)ccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915041 140448 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Br)ccc3c2n1 10.1016/j.bmcl.2011.08.014
24854637 196667 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc3ccccc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261363 196667 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 320 3 0 5 3.2 CN1CCN(c2nc3ccccc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
11738520 276589 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1O2 10.1021/jm051008s
CHEMBL379044 276589 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1O2 10.1021/jm051008s
60150162 347942 3 None -257 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4539444 347942 3 None -257 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
164624107 369010 0 None -70 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 369010 0 None -70 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
164608941 367696 0 None -75 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4845733 367696 0 None -75 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
57392890 140587 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 370 7 1 5 2.5 COc1cccc(C(O)(COc2ccccc2C)CN2CCN(C)CC2)c1 10.1016/j.bmcl.2011.07.114
CHEMBL1916492 140587 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 370 7 1 5 2.5 COc1cccc(C(O)(COc2ccccc2C)CN2CCN(C)CC2)c1 10.1016/j.bmcl.2011.07.114
135350581 426872 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 4 1 6 3.0 CC(C)N(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C(F)(F)F nan
CHEMBL5869362 426872 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 4 1 6 3.0 CC(C)N(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C(F)(F)F nan
21029584 372042 4 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncnc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL506969 372042 4 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncnc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
1267 8287 36 None -28 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
3035905 8287 36 None -28 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
CHEMBL260374 8287 36 None -28 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
90655029 219675 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 273 2 2 5 1.4 Nc1nc(C2CCCC2)cc(N2C[C@@H]3CNC[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3236563 219675 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 273 2 2 5 1.4 Nc1nc(C2CCCC2)cc(N2C[C@@H]3CNC[C@@H]3C2)n1 10.1021/jm401727m
71518862 177375 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 342 2 2 5 2.6 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314775 177375 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 342 2 2 5 2.6 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
44547567 235974 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393533 235974 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
24826163 140437 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915020 140437 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
57393773 140450 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 1 7 1.8 CN1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1915044 140450 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 1 7 1.8 CN1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
11572877 139367 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL187285 139367 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
44129210 431381 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 7 2 7 1.4 CNS(=O)(=O)CCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591711 431381 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 7 2 7 1.4 CNS(=O)(=O)CCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
156015638 352187 0 None -37 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 352187 0 None -37 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
25179127 372237 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL509852 372237 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25179127 372237 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL509852 372237 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
71518863 177376 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 338 3 2 6 2.0 COc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
CHEMBL2314776 177376 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 338 3 2 6 2.0 COc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
135353285 428515 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 418 5 1 6 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cccnn1)c1ccnc(N)n1 nan
CHEMBL5888593 428515 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 418 5 1 6 5.2 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cccnn1)c1ccnc(N)n1 nan
8070960 311629 8 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 258 2 0 5 1.4 COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL405044 311629 8 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 258 2 0 5 1.4 COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
25130576 370860 0 None -8 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130576 370860 0 None -8 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 370860 0 None -8 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 370860 0 None -8 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
86277887 251873 32 None None None Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 802 18 0 11 7.4 COc1ccc(CC[C@@H](OC(=O)[C@@H]2CCCCN2C(=O)[C@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC 10.6019/CHEMBL5058648
CHEMBL3623630 251873 32 None None None Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 802 18 0 11 7.4 COc1ccc(CC[C@@H](OC(=O)[C@@H]2CCCCN2C(=O)[C@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC 10.6019/CHEMBL5058648
168294445 385555 0 None -31 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 385555 0 None -31 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
135353283 447762 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 6 1 6 3.3 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)CC)cc1C1CCC1 nan
CHEMBL5986820 447762 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 6 1 6 3.3 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)CC)cc1C1CCC1 nan
135353332 463577 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 359 4 1 6 3.5 Cc1cc(Br)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6051052 463577 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 359 4 1 6 3.5 Cc1cc(Br)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
25130235 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
46228076 465609 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 354 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(C(C)(C)C)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL608864 465609 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 354 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(C(C)(C)C)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46228158 465674 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL609289 465674 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
57402514 140446 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Br)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915039 140446 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Br)cc3c2n1 10.1016/j.bmcl.2011.08.014
164619039 369425 0 None -17 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872277 369425 0 None -17 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
57392889 140586 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 379 4 1 5 2.2 CN1CCN(c2cc(C(=O)NCc3cccc(C(F)(F)F)c3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916491 140586 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 379 4 1 5 2.2 CN1CCN(c2cc(C(=O)NCc3cccc(C(F)(F)F)c3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
135353328 405832 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 320 3 1 4 3.7 Cc1cc(Br)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5749301 405832 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 320 3 1 4 3.7 Cc1cc(Br)ccc1N(c1ccnc(N)n1)C(C)C nan
135353334 431890 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 5 1 6 3.3 CC(C)N(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
CHEMBL5922399 431890 0 None None None Human 7.5 pKi = 7.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 360 5 1 6 3.3 CC(C)N(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
25130235 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 370821 1 None 1 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
57393774 140451 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.4 Nc1nc(N2CCNCC2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915045 140451 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.4 Nc1nc(N2CCNCC2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
10083188 278200 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL382276 278200 2 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
1279 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
4908365 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
CHEMBL129198 7960 58 None -3 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
71603137 180545 0 None 23 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 1 2 5 1.9 CC(C)(C)c1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376791 180545 0 None 23 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 1 2 5 1.9 CC(C)(C)c1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25179125 372183 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL509142 372183 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179125 372183 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL509142 372183 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
127051047 277599 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806162 277599 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
7015108 444115 6 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 343 3 0 7 1.7 CN1CCN(c2ncnc3c2nnn3Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594729 444115 6 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 343 3 0 7 1.7 CN1CCN(c2ncnc3c2nnn3Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2009.08.059
46228070 433106 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 271 4 0 5 1.1 CN1CCN(Cc2cn(Cc3ccccc3)nn2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593448 433106 0 None None None Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 271 4 0 5 1.1 CN1CCN(Cc2cn(Cc3ccccc3)nn2)CC1 10.1016/j.bmc.2009.08.059
135353275 410125 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 451 6 1 7 3.8 CCc1cc(S(C)(=O)=O)ccc1N(Cc1cccc(C(F)(F)F)n1)c1ccnc(N)n1 nan
CHEMBL5792923 410125 0 None None None Human 6.5 pKi = 6.5 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 451 6 1 7 3.8 CCc1cc(S(C)(=O)=O)ccc1N(Cc1cccc(C(F)(F)F)n1)c1ccnc(N)n1 nan
122193100 251973 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 314 3 1 6 1.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628047 251973 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 314 3 1 6 1.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
155513612 350289 0 None 4 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None 4 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
127050018 270583 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 221 2 2 5 0.5 CN[C@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1039/C6MD00108D
CHEMBL3818402 270583 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 221 2 2 5 0.5 CN[C@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1039/C6MD00108D
24994950 219693 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.5 CN[C@@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1021/jm401727m
CHEMBL3236580 219693 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.5 CN[C@@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1021/jm401727m
54583875 124313 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770995 124313 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
90655028 219669 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236557 219669 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@H](N)C2)n1 10.1021/jm401727m
59777262 219684 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236572 219684 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
155512725 350210 0 None 154 2 Human 7.4 pKi = 7.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 350210 0 None 154 2 Human 7.4 pKi = 7.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
46929553 40637 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243366 40637 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
71519011 177341 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 376 2 2 5 3.3 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)c(Cl)c4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314496 177341 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 376 2 2 5 3.3 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)c(Cl)c4)cc23)CC1 10.1016/j.bmcl.2012.10.139
24826598 140440 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 2 7 1.9 COc1ccc2oc3c(N4CCC[C@H](N)C4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1915027 140440 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 2 7 1.9 COc1ccc2oc3c(N4CCC[C@H](N)C4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
25178939 370113 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm800876b
CHEMBL489464 370113 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm800876b
24853529 196477 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 336 3 0 5 3.5 CN1CCN(c2nc3ccccc3nc2Sc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260388 196477 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 336 3 0 5 3.5 CN1CCN(c2nc3ccccc3nc2Sc2ccccc2)CC1 10.1021/jm7014217
25178939 370113 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm901379s
CHEMBL489464 370113 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm901379s
164611757 368209 0 None -50 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 368209 0 None -50 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
112936357 274762 0 None -18 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752978 274762 0 None -18 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
71519346 177365 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 232 1 2 6 -0.0 Cn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314764 177365 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 232 1 2 6 -0.0 Cn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
58227144 235996 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2cnnc(NC3CC4CCC3C4)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393555 235996 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2cnnc(NC3CC4CCC3C4)c2)CC1 10.1016/j.bmcl.2014.12.027
135353365 427540 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 384 6 1 5 4.8 COCCN(c1ccnc(N)n1)c1ccc(S(F)(F)(F)(F)F)cc1C nan
CHEMBL5877288 427540 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 384 6 1 5 4.8 COCCN(c1ccnc(N)n1)c1ccc(S(F)(F)(F)(F)F)cc1C nan
135353320 433204 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 477 6 1 7 4.5 CS(=O)(=O)c1ccc(N(Cc2cccc(C(F)(F)F)n2)c2ccnc(N)n2)c(C2CCC2)c1 nan
CHEMBL5935476 433204 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 477 6 1 7 4.5 CS(=O)(=O)c1ccc(N(Cc2cccc(C(F)(F)F)n2)c2ccnc(N)n2)c(C2CCC2)c1 nan
57399018 140453 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 332 1 1 7 2.1 CN1CCCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1915047 140453 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 332 1 1 7 2.1 CN1CCCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
16082831 155181 0 None -10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL214311 155181 0 None -10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
25178554 347524 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm800876b
CHEMBL452870 347524 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm800876b
25178554 347524 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm901379s
CHEMBL452870 347524 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm901379s
164610892 368496 0 None -52 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 368496 0 None -52 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
71518864 177377 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 322 2 2 5 2.3 Cc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
CHEMBL2314777 177377 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 322 2 2 5 2.3 Cc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
122194626 252071 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1ccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2015.08.014
CHEMBL3629829 252071 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1ccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2015.08.014
57399019 140457 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 2 2 7 1.4 NCC1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915051 140457 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 2 2 7 1.4 NCC1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
90645146 221664 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 288 2 1 6 1.0 CN1CCN(c2nc(N)nc(-c3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290577 221664 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 288 2 1 6 1.0 CN1CCN(c2nc(N)nc(-c3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
54584374 125841 0 None -6 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789360 125841 0 None -6 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
122193105 251977 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628051 251977 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2015.08.014
135353316 413508 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 427 6 1 8 3.2 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
CHEMBL5830658 413508 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 427 6 1 8 3.2 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
921599 43307 47 None 660 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0341047
CHEMBL129660 43307 47 None 660 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0341047
921599 43307 47 None 660 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0502081
CHEMBL129660 43307 47 None 660 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0502081
4060730 43234 34 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL129199 43234 34 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.02.097
25178553 347523 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm800876b
CHEMBL452869 347523 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm800876b
25178553 347523 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm901379s
CHEMBL452869 347523 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm901379s
11846465 279116 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
CHEMBL387054 279116 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
56851606 143828 0 None -11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 432 8 2 3 5.7 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1963244 143828 0 None -11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 432 8 2 3 5.7 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
51354877 121693 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCc2cn(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688988 121693 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 7 1 4 3.1 c1nc(CCCc2cn(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
137658819 315157 0 None -7585 2 Human 5.4 pKi = 5.4 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 467 9 1 5 3.9 COc1cc2c(cc1OC)C(C)=C(C(=O)NCCCCN1CCN(c3ccccc3F)CC1)C2 10.1016/j.ejmech.2016.09.074
CHEMBL4099779 315157 0 None -7585 2 Human 5.4 pKi = 5.4 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 467 9 1 5 3.9 COc1cc2c(cc1OC)C(C)=C(C(=O)NCCCCN1CCN(c3ccccc3F)CC1)C2 10.1016/j.ejmech.2016.09.074
54584374 125841 0 None -6 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789360 125841 0 None -6 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
58227207 235992 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393551 235992 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
51354872 122971 0 None -323 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 291 6 0 5 2.1 c1c(CN2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
CHEMBL1739923 122971 0 None -323 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 291 6 0 5 2.1 c1c(CN2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
135353288 445417 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 5 1 6 2.9 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
CHEMBL5961050 445417 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 5 1 6 2.9 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CCC1 nan
135353277 463025 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 6 1 7 3.8 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ccncc1F)c1ccnc(N)n1 nan
CHEMBL6045476 463025 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 6 1 7 3.8 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ccncc1F)c1ccnc(N)n1 nan
58227381 350579 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 nan
CHEMBL4597817 350579 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 nan
68081433 219663 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 248 1 1 3 0.7 CN1CCN(C(=O)c2nc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
CHEMBL3236551 219663 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 248 1 1 3 0.7 CN1CCN(C(=O)c2nc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
57399747 140408 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 2 2 6 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914787 140408 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 2 2 6 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)C1 10.1016/j.bmcl.2011.08.014
25129169 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
25129169 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL492231 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
3032915 39388 20 None -1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 39388 20 None -1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681806 180474 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 331 8 4 9 1.0 CC(C)CNc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375667 180474 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 331 8 4 9 1.0 CC(C)CNc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681639 180491 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 321 6 3 7 2.3 Cc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375762 180491 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 321 6 3 7 2.3 Cc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
11492393 8807 7 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
1263 8807 7 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
CHEMBL206346 8807 7 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
11557610 156123 0 None -10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 7 2 2 2.7 c1nc(CCCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL202744 156123 0 None -10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 7 2 2 2.7 c1nc(CCCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
11615406 276809 1 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 6 2 2 2.3 c1nc(CCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL379447 276809 1 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 6 2 2 2.3 c1nc(CCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
66572116 157325 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 2 2 1.5 Cc1cccc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047443 157325 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 2 2 1.5 Cc1cccc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
70681961 157337 2 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 1 1 2 2.6 CN1CCCN(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047455 157337 2 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 1 1 2 2.6 CN1CCCN(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70696621 157344 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 287 2 1 2 2.2 O=C(c1cc2cccc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047462 157344 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 287 2 1 2 2.2 O=C(c1cc2cccc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
70692531 157357 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.0 Cc1ccc(F)c2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047475 157357 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.0 Cc1ccc(F)c2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24759623 196695 15 None 18 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm800876b
CHEMBL261551 196695 15 None 18 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm800876b
25129169 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 370430 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
24759623 196695 15 None 18 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261551 196695 15 None 18 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
10429016 392732 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 366 7 3 3 3.6 N=C(NCCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL561250 392732 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 366 7 3 3 3.6 N=C(NCCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1223 1963 35 None -21 8 Human 7.4 pKi = 7.4 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.4 pKi = 7.4 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.4 pKi = 7.4 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
71519012 177342 0 None 218 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.8 Nc1nc(N2CCNCC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314497 177342 0 None 218 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.8 Nc1nc(N2CCNCC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
10934158 212958 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 212958 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
71681478 180488 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 392 9 4 8 3.2 CC(C)CCc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375759 180488 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 392 9 4 8 3.2 CC(C)CCc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
11629829 157681 0 None -19 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205583 157681 0 None -19 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
25831 27269 8 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 144 3 6 2 -2.0 N=C(N)NCCNC(=N)N 10.1021/jm060880d
CHEMBL1189742 27269 8 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 144 3 6 2 -2.0 N=C(N)NCCNC(=N)N 10.1021/jm060880d
1279 7960 58 None -3 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 7960 58 None -3 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 7960 58 None -3 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
66573456 157327 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 2 2 2 1.5 CNC1CN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047445 157327 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 2 2 2 1.5 CNC1CN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
43398194 157338 23 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 CN1CCCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047456 157338 23 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 CN1CCCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70694582 157342 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047460 157342 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70686223 157347 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 2 2 2 1.4 CNC1CN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047465 157347 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 2 2 2 1.4 CNC1CN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
70692530 157356 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047474 157356 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1238 4258 10 None -35 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 4258 10 None -35 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 4258 10 None -35 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
44417445 27067 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 217 7 5 3 0.7 N=C(N)NCCCCCCSC(=N)N 10.1021/jm060880d
CHEMBL1188154 27067 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 217 7 5 3 0.7 N=C(N)NCCCCCCSC(=N)N 10.1021/jm060880d
66572102 157299 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ncccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047260 157299 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ncccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
24854634 312080 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 400 4 0 4 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2CCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL406379 312080 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 400 4 0 4 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2CCc2ccccc2)CC1 10.1021/jm7014217
24853528 331882 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 329 6 0 6 1.7 CN(C)CCCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL428964 331882 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 329 6 0 6 1.7 CN(C)CCCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
137659490 315047 0 None 11 2 Human 8.4 pKi = 8.4 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 420 7 1 2 6.1 Brc1ccc(C(OCCCc2c[nH]cn2)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4098585 315047 0 None 11 2 Human 8.4 pKi = 8.4 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 420 7 1 2 6.1 Brc1ccc(C(OCCCc2c[nH]cn2)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2016.09.074
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
135350871 462968 0 None None None Human 8.4 pKi = 8.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 338 5 1 4 4.6 CCCc1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL6045066 462968 0 None None None Human 8.4 pKi = 8.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 338 5 1 4 4.6 CCCc1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
24803709 292644 1 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cc(F)cc2[nH]1 nan
CHEMBL3917992 292644 1 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cc(F)cc2[nH]1 nan
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
49841846 141986 0 None 18 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 141986 0 None 18 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
44129130 432014 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL592379 432014 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.10.104
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
24745337 124297 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770979 124297 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227340 235973 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393532 235973 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2023.115151
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2023.115151
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2023.115151
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 7960 58 None 3 7 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None 3 7 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None 3 7 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
44129133 430700 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 398 6 2 7 1.0 CNS(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591011 430700 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 398 6 2 7 1.0 CNS(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
1223 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
2790 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
CHEMBL14690 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
1223 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
2790 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
CHEMBL14690 1963 35 None -21 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
25129169 370430 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL492231 370430 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
44129134 431638 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 431638 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25129169 370430 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 370430 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
1279 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
4908365 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
CHEMBL129198 7960 58 None -3 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
24745506 140490 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915537 140490 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
136042266 142157 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938975 142157 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
136042268 142159 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938977 142159 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
25068753 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1279 7960 58 None 3 7 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
4908365 7960 58 None 3 7 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
CHEMBL129198 7960 58 None 3 7 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
25068753 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
2063135 22692 6 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1093180 22692 6 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
24826437 140369 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@H]3CCCN[C@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914746 140369 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@H]3CCCN[C@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25128823 385260 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 385260 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
58227193 431090 0 None None None Human 8.3 pKi = 8.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 275 4 2 5 2.0 CN[C@@H]1CCN(c2cnnc(NC3CCCCC3)c2)C1 nan
CHEMBL5914057 431090 0 None None None Human 8.3 pKi = 8.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 275 4 2 5 2.0 CN[C@@H]1CCN(c2cnnc(NC3CCCCC3)c2)C1 nan
25129527 370651 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.ejmech.2023.115151
CHEMBL493720 370651 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.ejmech.2023.115151
1247 7944 80 None -12 11 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 7944 80 None -12 11 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 7944 80 None -12 11 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 7944 80 None -12 11 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
11957573 4107 26 None -7 7 Human 8.3 pKi = 8.3 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.6019/CHEMBL5442175
1250 4107 26 None -7 7 Human 8.3 pKi = 8.3 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.6019/CHEMBL5442175
3692 4107 26 None -7 7 Human 8.3 pKi = 8.3 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.6019/CHEMBL5442175
CHEMBL19439 4107 26 None -7 7 Human 8.3 pKi = 8.3 Binding
PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.6019/CHEMBL5442175
1279 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
4908365 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
CHEMBL129198 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
44129130 432014 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 432014 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
921599 43307 47 None 660 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2023.115151
CHEMBL129660 43307 47 None 660 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2023.115151
135353280 432797 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 286 4 1 4 3.8 C=C(C)c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5931224 432797 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 286 4 1 4 3.8 C=C(C)c1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
54581941 124315 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 288 2 2 6 0.8 Nc1nc(N2CCCC2)cc(N2CC3CCCNC3C2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770997 124315 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 288 2 2 6 0.8 Nc1nc(N2CCCC2)cc(N2CC3CCCNC3C2)n1 10.1016/j.bmcl.2011.03.017
24826680 140399 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914777 140399 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
11601630 260678 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL370135 260678 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
137640214 312879 0 None None None Human 6.4 pKi = 6.4 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 394 6 1 2 5.5 O=C(NCCCCN1Cc2cccc3cccc(c23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2016.09.074
CHEMBL4072893 312879 0 None None None Human 6.4 pKi = 6.4 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 394 6 1 2 5.5 O=C(NCCCCN1Cc2cccc3cccc(c23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2016.09.074
71519013 177343 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 3 2 5 2.5 CCN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314498 177343 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 3 2 5 2.5 CCN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
168284289 385450 0 None -37 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 385450 0 None -37 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
3076002 353175 2 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL473099 353175 2 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
3076002 353175 2 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL473099 353175 2 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
90645150 221660 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290573 221660 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
135353292 406909 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 429 5 1 7 4.0 Nc1nccc(N(Cc2cocn2)c2ccc(Br)cc2OC(F)(F)F)n1 nan
CHEMBL5760335 406909 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 429 5 1 7 4.0 Nc1nccc(N(Cc2cocn2)c2ccc(Br)cc2OC(F)(F)F)n1 nan
25130576 370860 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130576 370860 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 370860 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 370860 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
10018335 144235 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL197477 144235 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
57393771 140445 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 311 2 2 7 1.5 COc1ccc2oc3c(N4C[C@@H]5C[C@H]4CN5)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1915035 140445 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 311 2 2 7 1.5 COc1ccc2oc3c(N4C[C@@H]5C[C@H]4CN5)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
10545988 125864 0 None -93 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789558 125864 0 None -93 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
46228071 445819 12 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596562 445819 12 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmc.2009.08.059
135350545 411480 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 348 6 1 6 2.8 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1CC(C)C nan
CHEMBL5808012 411480 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 348 6 1 6 2.8 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1CC(C)C nan
1247 7944 80 None -199 11 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 7944 80 None -199 11 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 7944 80 None -199 11 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 7944 80 None -199 11 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
46890590 21353 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084810 21353 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57400735 140439 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 2 6 2.9 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915026 140439 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 2 6 2.9 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
58227346 413119 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 263 3 2 6 0.6 N[C@@H]1CCN(c2ccnc(NC3CCOCC3)n2)C1 nan
CHEMBL5826331 413119 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 263 3 2 6 0.6 N[C@@H]1CCN(c2ccnc(NC3CCOCC3)n2)C1 nan
56851441 143827 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 7 2 3 4.2 c1ccc(CN/C(=N/C2CCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963243 143827 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 7 2 3 4.2 c1ccc(CN/C(=N/C2CCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
25147772 347506 9 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL452847 347506 9 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
16061961 432771 0 None 7 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 432771 0 None 7 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10381810 470034 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL7828 470034 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
137647794 313865 0 None None None Human 5.4 pKi = 5.4 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 464 8 1 6 4.2 COc1ccc2c(c1)c(CC(=O)NCCCn1ccnc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4085023 313865 0 None None None Human 5.4 pKi = 5.4 Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 464 8 1 6 4.2 COc1ccc2c(c1)c(CC(=O)NCCCn1ccnc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
10545988 125864 0 None -93 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789558 125864 0 None -93 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
122193096 251969 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628043 251969 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645154 221668 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 338 2 1 6 1.9 CN1CCN(c2nc(N)nc(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290581 221668 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 338 2 1 6 1.9 CN1CCN(c2nc(N)nc(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
135353314 424171 0 None None None Human 6.4 pKi = 6.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 373 6 1 8 2.5 CCS(=O)(=O)c1ccc(N(Cc2cocn2)c2ccnc(N)n2)c(C)c1 nan
CHEMBL5839966 424171 0 None None None Human 6.4 pKi = 6.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 373 6 1 8 2.5 CCS(=O)(=O)c1ccc(N(Cc2cocn2)c2ccnc(N)n2)c(C)c1 nan
10777275 20226 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.6 CCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079553 20226 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.6 CCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
1267 8287 36 None -28 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
3035905 8287 36 None -28 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
CHEMBL260374 8287 36 None -28 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
127036978 274686 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752225 274686 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
164612037 368668 0 None -954 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 368668 0 None -954 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
10660 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
1224 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
3100 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
441281 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
8980 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
916 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
CHEMBL1200406 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
CHEMBL657 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB00985 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB01075 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB13636 2953 69 None -77 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
9883231 232434 1 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 312 1 1 3 2.0 CN1CCN(C(=O)c2nc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL331773 232434 1 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 312 1 1 3 2.0 CN1CCN(C(=O)c2nc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
1267 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
3035905 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
CHEMBL260374 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
1267 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
3035905 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
CHEMBL260374 8287 36 None -28 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
24992735 219695 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
CHEMBL3236582 219695 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
24826081 140384 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914762 140384 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.08.014
90645153 221667 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 284 2 1 6 1.2 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2014.06.032
CHEMBL3290580 221667 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 284 2 1 6 1.2 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2014.06.032
25178344 370145 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489664 370145 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10934158 212958 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 212958 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
24853593 196413 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccncc2)CC1 10.1021/jm7014217
CHEMBL259956 196413 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccncc2)CC1 10.1021/jm7014217
135353368 448152 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 6 1 6 2.9 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CC1 nan
CHEMBL5990927 448152 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 346 6 1 6 2.9 CCCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CC1 nan
54586765 124300 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(NCCO)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770982 124300 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(NCCO)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
44275465 199440 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2013.02.091
CHEMBL281590 199440 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2013.02.091
24826080 140386 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 1 1 6 3.2 CN1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914764 140386 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 1 1 6 3.2 CN1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)CC1 10.1016/j.bmcl.2011.08.014
71519349 177368 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 326 2 2 6 1.8 Cn1c(-c2ccc(F)cc2)cc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314767 177368 0 None None None Human 4.4 pKi = 4.4 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 326 2 2 6 1.8 Cn1c(-c2ccc(F)cc2)cc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
57393770 140442 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915031 140442 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
155534519 350450 0 None -47 2 Human 6.4 pKi = 6.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 288 7 3 5 2.7 CC(C)(C)CNc1nccc(NCCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596640 350450 0 None -47 2 Human 6.4 pKi = 6.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 288 7 3 5 2.7 CC(C)(C)CNc1nccc(NCCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
51354873 121690 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 267 6 1 4 2.2 c1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688984 121690 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 267 6 1 4 2.2 c1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
51354874 121691 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 335 6 1 4 3.5 Clc1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1Cl 10.1021/jm1013488
CHEMBL1688985 121691 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 335 6 1 4 3.5 Clc1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1Cl 10.1021/jm1013488
168292954 385542 0 None -69 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 385542 0 None -69 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
11779175 125882 0 None -5 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789801 125882 0 None -5 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164612760 368027 0 None -38 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4850490 368027 0 None -38 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
11779175 125882 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789801 125882 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
135350610 427668 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 313 6 2 5 2.5 CCN(c1ccnc(N)n1)c1ccc(C(N)=O)cc1CC(C)C nan
CHEMBL5878819 427668 0 None None None Human 7.4 pKi = 7.4 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 313 6 2 5 2.5 CCN(c1ccnc(N)n1)c1ccc(C(N)=O)cc1CC(C)C nan
58227085 235986 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393545 235986 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
44546971 406686 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 4 2 4 1.6 CC(C)CNc1cc(N2CCNCC2)ccn1 nan
CHEMBL5757988 406686 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 4 2 4 1.6 CC(C)CNc1cc(N2CCNCC2)ccn1 nan
1267 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
3035905 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
CHEMBL260374 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
11846464 160015 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
CHEMBL211170 160015 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
118720433 234845 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 206 3 1 4 0.8 CCc1cc(N2CC[C@@H](NC)C2)ncn1 10.1016/j.bmcl.2014.10.013
CHEMBL3354807 234845 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 206 3 1 4 0.8 CCc1cc(N2CC[C@@H](NC)C2)ncn1 10.1016/j.bmcl.2014.10.013
51354581 121681 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 275 10 1 4 3.1 CCCCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688973 121681 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 275 10 1 4 3.1 CCCCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
9877454 470443 2 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL81644 470443 2 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
1613 4786 46 None -28 28 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 4786 46 None -28 28 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 4786 46 None -28 28 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 4786 46 None -28 28 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 4786 46 None -28 28 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
164609493 367746 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 367746 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
71518698 177370 0 None None None Human 4.3 pKi = 4.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 218 1 3 5 -0.1 Nc1nc(N2CCNCC2)c2cc[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314770 177370 0 None None None Human 4.3 pKi = 4.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 218 1 3 5 -0.1 Nc1nc(N2CCNCC2)c2cc[nH]c2n1 10.1016/j.bmcl.2012.10.139
4242975 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
CHEMBL128088 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
135350543 412794 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 415 6 1 6 3.8 CC(C)=Cc1cc(S(=O)(=O)N2CCCC2)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5822854 412794 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 415 6 1 6 3.8 CC(C)=Cc1cc(S(=O)(=O)N2CCCC2)ccc1N(c1ccnc(N)n1)C(C)C nan
135353298 463346 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 422 6 1 7 5.0 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1nnco1)c1ccnc(N)n1 nan
CHEMBL6048687 463346 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 422 6 1 7 5.0 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1nnco1)c1ccnc(N)n1 nan
4242975 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL128088 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
16061961 432771 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 432771 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
11258458 174456 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 412 6 1 4 4.5 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
CHEMBL219930 174456 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 412 6 1 4 4.5 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
57398183 140324 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 347 4 3 7 1.8 Nc1nc(N2CC[C@@H](NCCO)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914545 140324 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 347 4 3 7 1.8 Nc1nc(N2CC[C@@H](NCCO)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
4242975 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128088 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
58227230 407498 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 235 4 2 5 1.0 CC(C)CNc1nccc(N2CCNCC2)n1 nan
CHEMBL5766097 407498 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 235 4 2 5 1.0 CC(C)CNc1nccc(N2CCNCC2)n1 nan
118720438 234851 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 220 3 1 4 1.4 CN[C@@H]1CCN(c2ccnc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354814 234851 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 220 3 1 4 1.4 CN[C@@H]1CCN(c2ccnc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
24854640 196414 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccccn2)CC1 10.1021/jm7014217
CHEMBL259957 196414 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccccn2)CC1 10.1021/jm7014217
135589846 279013 1 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 356 2 2 5 3.1 OCCN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1021/jm051008s
CHEMBL386333 279013 1 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 356 2 2 5 3.1 OCCN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1021/jm051008s
24826439 140393 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 2 2 7 1.4 COc1cccc2oc3c(N4CCNCC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
CHEMBL1914771 140393 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 2 2 7 1.4 COc1cccc2oc3c(N4CCNCC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
10446295 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
1277 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL185951 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
10446295 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
1277 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL185951 4352 37 None 263 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
10023327 333639 0 None -144 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
1267 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
3035905 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
CHEMBL260374 8287 36 None -28 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
155556721 348601 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 248 2 1 6 0.6 CC(C)=Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4556243 348601 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 248 2 1 6 0.6 CC(C)=Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
24854639 196489 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 348 5 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260458 196489 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 348 5 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCCc2ccccc2)CC1 10.1021/jm7014217
11344458 470058 0 None -14 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78497 470058 0 None -14 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
51354588 122943 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 292 6 0 5 2.1 c1c(CC2CCCCC2)nnn1CCCN1CCOCC1 10.1021/jm1013488
CHEMBL1739759 122943 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 292 6 0 5 2.1 c1c(CC2CCCCC2)nnn1CCCN1CCOCC1 10.1021/jm1013488
16106 236970 34 None -23 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 10.1021/jm051008s
2111 236970 34 None -23 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 10.1021/jm051008s
CHEMBL340801 236970 34 None -23 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 10.1021/jm051008s
46881855 22065 0 None -15 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089040 22065 0 None -15 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
71519014 177344 0 None None None Human 4.3 pKi = 4.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 2 5 2.9 CC(C)N1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314499 177344 0 None None None Human 4.3 pKi = 4.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 2 5 2.9 CC(C)N1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
122193094 251967 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628041 251967 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
155513612 350289 0 None -4 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 350289 0 None -4 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
45379808 462091 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 362 5 2 6 1.6 CC(=O)NCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL603621 462091 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 362 5 2 6 1.6 CC(=O)NCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
168286426 385471 0 None -323 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 385471 0 None -323 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164620139 369073 0 None -56 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4866734 369073 0 None -56 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
136042267 142158 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938976 142158 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
11623296 235888 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338972 235888 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
135353339 462718 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cnoc1)c1ccnc(N)n1 nan
CHEMBL6042713 462718 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1cnoc1)c1ccnc(N)n1 nan
11066922 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129436 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
11066922 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL129436 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0341047
49841845 141987 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 141987 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
25068753 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.10.104
CHEMBL502347 371642 21 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.10.104
1223 1963 35 None -21 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
2790 1963 35 None -21 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
CHEMBL14690 1963 35 None -21 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
1279 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
1279 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
4908365 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
4908365 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
CHEMBL129198 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
CHEMBL129198 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
58227086 235998 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393557 235998 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1279 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
4908365 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
CHEMBL129198 7960 58 None -3 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
2063135 22692 6 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1021/jm401727m
CHEMBL1093180 22692 6 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1021/jm401727m
23650959 219661 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 410 7 1 4 5.3 Cc1cnc(OCCCCC2CCN(C)CC2)cc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/jm401727m
CHEMBL3236548 219661 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 410 7 1 4 5.3 Cc1cnc(OCCCCC2CCN(C)CC2)cc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/jm401727m
11066922 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129436 43275 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
155524115 350512 0 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 350512 0 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
70696620 157332 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 292 1 2 3 1.8 CN1CCN(C(=O)c2cc3cc(Cl)cc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047450 157332 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 292 1 2 3 1.8 CN1CCN(C(=O)c2cc3cc(Cl)cc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
25129523 370534 40 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 370534 40 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
76311195 215735 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 284 2 2 6 1.1 CN1CCN(c2cc(-c3ccc(N)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL3133130 215735 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 284 2 2 6 1.1 CN1CCN(c2cc(-c3ccc(N)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
25129523 370534 40 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 370534 40 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
25128824 385707 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 385707 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
155524115 350512 0 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 350512 0 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
25128824 385707 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 385707 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
25071004 385261 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 385261 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
11705395 39942 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
CHEMBL1223749 39942 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
24826162 140413 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914792 140413 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
71519674 180558 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 180558 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
46890072 21239 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084355 21239 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
24994634 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
24994634 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
8984 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL3236549 4374 36 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
44129056 432332 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 474 7 1 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592663 432332 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 474 7 1 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25128822 370716 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 370716 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
11554490 39943 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.ejmech.2016.09.074
CHEMBL1223750 39943 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.ejmech.2016.09.074
24797956 219670 1 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 219670 1 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
24825514 370117 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL489493 370117 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
24825515 370564 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL493014 370564 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
11301441 196507 12 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm800876b
CHEMBL260549 196507 12 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm800876b
11301441 196507 12 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL260549 196507 12 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm7014217
24825791 140327 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914548 140327 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25109291 366002 9 None -478 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 366002 9 None -478 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
45379922 432086 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 552 7 2 7 2.8 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(I)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592434 432086 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 552 7 2 7 2.8 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(I)ccc3n2)CC1 10.1021/jm901379s
117724514 451023 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 329 4 2 5 2.8 CN[C@@H]1CCN(c2cnnc(NC3C[C@H]4C[C@@H]([C@@H]3C)C4(C)C)c2)C1 nan
CHEMBL6021205 451023 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 329 4 2 5 2.8 CN[C@@H]1CCN(c2cnnc(NC3C[C@H]4C[C@@H]([C@@H]3C)C4(C)C)c2)C1 nan
54585777 124292 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 5 3 5 2.1 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770974 124292 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 5 3 5 2.1 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)c2)C1 10.1016/j.bmcl.2011.03.017
118720441 234855 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 3 4 2.5 Nc1cc(C2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354819 234855 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 3 4 2.5 Nc1cc(C2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
24826518 140375 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2cccc(C(F)(F)F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914753 140375 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2cccc(C(F)(F)F)c23)CC1 10.1016/j.bmcl.2011.08.014
1279 7960 58 None -3 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 7960 58 None -3 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 7960 58 None -3 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
136192886 119279 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632411 119279 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136141537 119280 6 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 119280 6 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
71525678 180554 0 None -4 6 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 180554 0 None -4 6 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
1267 8287 36 None -11 9 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
3035905 8287 36 None -11 9 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
CHEMBL260374 8287 36 None -11 9 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1269 249 35 None 213 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 249 35 None 213 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 249 35 None 213 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
1255 6493 23 None -12 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 6493 23 None -12 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 6493 23 None -12 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
10017000 469387 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL72431 469387 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 1963 35 None -21 8 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
71681644 180496 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 412 9 4 8 3.8 CC(C)CNc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375767 180496 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 412 9 4 8 3.8 CC(C)CNc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
71681805 180501 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 426 9 3 8 3.8 CC(C)CNc1nccc(NCCN(C)c2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375771 180501 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 426 9 3 8 3.8 CC(C)CNc1nccc(NCCN(C)c2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
11506928 156118 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 6 2 2 3.0 c1nc(CCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL202728 156118 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 235 6 2 2 3.0 c1nc(CCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
11600779 157707 0 None -6 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205731 157707 0 None -6 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
11536119 276062 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL377954 276062 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
4242975 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL128088 42701 7 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
45379921 429457 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 426 6 1 7 3.6 CN1CCN(c2nc(NCCc3ccc([N+](=O)[O-])cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL589800 429457 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 426 6 1 7 3.6 CN1CCN(c2nc(NCCc3ccc([N+](=O)[O-])cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
9972181 389979 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 8 3 3 3.2 N=C(NCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL550757 389979 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 8 3 3 3.2 N=C(NCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10063835 125840 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789356 125840 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
46890200 21482 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 442 9 1 4 5.4 CN(C)CCN(C)CCCOc1ccc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)cc1Cl 10.1016/j.bmcl.2010.04.017
CHEMBL1085403 21482 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 442 9 1 4 5.4 CN(C)CCN(C)CCCOc1ccc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)cc1Cl 10.1016/j.bmcl.2010.04.017
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -199 11 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -199 11 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -199 11 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -199 11 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
71681803 180445 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)ncn1 10.1021/jm301886t
CHEMBL2375363 180445 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)ncn1 10.1021/jm301886t
11672774 8809 11 None -31 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
1245 8809 11 None -31 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
CHEMBL206548 8809 11 None -31 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
11564628 157197 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL204360 157197 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
11629931 157969 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205868 157969 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
70686222 157346 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 2 2 2 1.7 CN[C@@H]1CCN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047464 157346 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 261 2 2 2 1.7 CN[C@@H]1CCN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
135398737 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
2818 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
38 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
722 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
CHEMBL253391 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
CHEMBL42 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
DB00363 1973 61 None -57 61 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
44395314 251758 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL362163 251758 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
126688 835 21 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
4025 835 21 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
CHEMBL293762 835 21 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
66572110 157308 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 1 3 1.8 CC(=O)c1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
CHEMBL2047269 157308 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 285 2 1 3 1.8 CC(=O)c1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
70684085 157339 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 325 1 1 2 3.0 CN1CCCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047457 157339 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 325 1 1 2 3.0 CN1CCCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10063835 125840 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789356 125840 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
206876 42802 4 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1039/C2MD20212C
CHEMBL128637 42802 4 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1039/C2MD20212C
57395620 140487 0 None 15 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915534 140487 0 None 15 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
57395620 140487 0 None 15 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915534 140487 0 None 15 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
90645160 221674 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3c(F)cccc3F)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290587 221674 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3c(F)cccc3F)n2)CC1 10.1016/j.ejmech.2014.06.032
57390145 142152 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938970 142152 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
49865668 39941 0 None -51 4 Human 7.3 pKi = 7.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.ejmech.2016.09.074
CHEMBL1223748 39941 0 None -51 4 Human 7.3 pKi = 7.3 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.ejmech.2016.09.074
54586764 124296 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N(C)C(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770978 124296 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N(C)C(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
44546966 235966 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393525 235966 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
44546966 235966 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 nan
CHEMBL3393525 235966 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 nan
9964223 470510 6 None -36 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL82244 470510 6 None -36 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
90645148 221662 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290575 221662 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
56950378 142114 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938845 142114 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
25071940 370596 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 370596 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
90645145 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL3290578 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
66741667 219678 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3236566 219678 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
122194623 252068 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 296 3 1 6 1.4 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3629826 252068 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 296 3 1 6 1.4 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645145 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
CHEMBL3290578 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
90645145 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290578 221665 0 None 28 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
10083861 39400 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 1 3 1.3 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)nc2c1 10.1021/jm0502081
CHEMBL121679 39400 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 1 3 1.3 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)nc2c1 10.1021/jm0502081
121238067 331909 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4290148 331909 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
135353370 446336 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 6 1 8 3.9 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1c(C)noc1C)c1ccnc(N)n1 nan
CHEMBL5970964 446336 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 455 6 1 8 3.9 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1c(C)noc1C)c1ccnc(N)n1 nan
57394636 140318 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 284 1 0 5 2.6 CN1CCN(c2ncnc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914534 140318 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 284 1 0 5 2.6 CN1CCN(c2ncnc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
71525587 180556 0 None 177 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 255 2 2 7 -0.1 CNC1CN(c2nc(N)nc3cc(C#N)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376802 180556 0 None 177 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 255 2 2 7 -0.1 CNC1CN(c2nc(N)nc3cc(C#N)cnc23)C1 10.1016/j.bmcl.2013.02.091
753256 353242 8 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL473662 353242 8 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmcl.2012.10.139
46228143 445184 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595880 445184 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
135353363 445115 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
CHEMBL5958104 445115 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 329 6 1 7 2.9 CCOc1cc(F)ccc1N(Cc1ncco1)c1ccnc(N)n1 nan
44547126 235968 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 nan
CHEMBL3393527 235968 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 nan
24745335 607 14 None -8 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 607 14 None -8 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 607 14 None -8 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 607 14 None -8 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
24745335 607 14 None -6 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 607 14 None -6 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 607 14 None -6 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 607 14 None -6 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
51354583 121683 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 6 1 4 3.1 c1nc(CCCn2cc(CC3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688975 121683 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 287 6 1 4 3.1 c1nc(CCCn2cc(CC3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
71518860 177373 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 308 2 2 5 2.0 CN1CCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314773 177373 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 308 2 2 5 2.0 CN1CCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
46228113 465581 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 328 5 2 7 1.4 COc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL608717 465581 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 328 5 2 7 1.4 COc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
164611807 368288 0 None -162 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4854278 368288 0 None -162 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
49841718 141983 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 349 3 1 6 2.6 COc1ccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)cc1 10.1016/j.bmcl.2011.10.104
CHEMBL1935569 141983 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 349 3 1 6 2.6 COc1ccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)cc1 10.1016/j.bmcl.2011.10.104
58227143 235982 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393541 235982 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
67087450 235991 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393550 235991 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
46890071 21238 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.7 Cc1cc(OCCCNCC2CCCN(C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084354 21238 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.7 Cc1cc(OCCCNCC2CCCN(C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
66740470 219355 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3233048 219355 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
2306318 177884 10 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL232421 177884 10 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
121238068 313118 0 None -281 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4076046 313118 0 None -281 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.09.035
25178341 370072 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489271 370072 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178341 370072 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489271 370072 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25178556 372243 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL509961 372243 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
23649429 196645 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 326 2 0 5 2.7 COc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL261224 196645 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 326 2 0 5 2.7 COc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
44478385 20108 8 None 9 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 20108 8 None 9 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
25178344 370145 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489664 370145 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
24853597 196644 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 3 0 5 3.5 Cc1cccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)c1 10.1021/jm7014217
CHEMBL261223 196644 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 334 3 0 5 3.5 Cc1cccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)c1 10.1021/jm7014217
8070044 311879 9 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 300 4 0 5 2.4 CC(C)COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL406123 311879 9 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 300 4 0 5 2.4 CC(C)COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
16061844 124299 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(NCc3ccccc3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770981 124299 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(NCc3ccccc3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
57403351 140594 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2cc(NCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
CHEMBL1916499 140594 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2cc(NCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
156011443 352256 0 None -50 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 387 8 1 2 4.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4651225 352256 0 None -50 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 387 8 1 2 4.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
25178339 370046 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489061 370046 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354585 121685 0 None -5 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 245 5 1 4 2.0 c1nc(CCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688977 121685 0 None -5 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 245 5 1 4 2.0 c1nc(CCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
51354876 122972 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.4 c1nc(CCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1739924 122972 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.4 c1nc(CCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
12741697 196513 2 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
CHEMBL260565 196513 2 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
25178339 370046 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489061 370046 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
919019 274161 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2[nH]c3c(N4CCN(C)CC4)ncnc3c2c1 10.1039/C5MD00022J
CHEMBL3740837 274161 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2[nH]c3c(N4CCN(C)CC4)ncnc3c2c1 10.1039/C5MD00022J
929854 427932 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 289 4 2 4 2.7 CN(C)CCNc1ncnc2c1[nH]c1ccc(Cl)cc12 10.1039/C5MD00022J
CHEMBL588176 427932 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 289 4 2 4 2.7 CN(C)CCNc1ncnc2c1[nH]c1ccc(Cl)cc12 10.1039/C5MD00022J
168278543 385395 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 385395 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168295803 385588 0 None -38 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 385588 0 None -38 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
57402471 140148 1 None -34 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910378 140148 1 None -34 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
164614645 368432 0 None -57 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 368432 0 None -57 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
135350838 409899 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 311 5 2 5 2.6 CCN(c1ccnc(N)n1)c1ccc(C(N)=O)cc1C1CCC1 nan
CHEMBL5790640 409899 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 311 5 2 5 2.6 CCN(c1ccnc(N)n1)c1ccc(C(N)=O)cc1C1CCC1 nan
57394627 140592 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 5 2 5 2.4 CN1CC[C@H](Nc2cc(NCCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
CHEMBL1916497 140592 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 5 2 5 2.4 CN1CC[C@H](Nc2cc(NCCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
71519179 177363 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 3 4 5 2.1 Nc1nc(N[C@H]2CCNC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314762 177363 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 3 4 5 2.1 Nc1nc(N[C@H]2CCNC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
135353289 432257 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 290 5 1 5 3.1 CCOc1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5925897 432257 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 290 5 1 5 3.1 CCOc1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
1247 7944 80 None -4 11 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 7944 80 None -4 11 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 7944 80 None -4 11 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 7944 80 None -4 11 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1279 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
1279 7960 58 None 3 7 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 7960 58 None 3 7 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 7960 58 None 3 7 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
44538833 141967 17 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@H]2CCCC[C@H]2O1 10.1016/j.bmcl.2011.10.104
CHEMBL1935450 141967 17 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@H]2CCCC[C@H]2O1 10.1016/j.bmcl.2011.10.104
49841719 141985 0 None 38 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 141985 0 None 38 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
11846300 161722 3 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL213912 161722 3 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2011.10.104
11301441 196507 12 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL260549 196507 12 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1016/j.bmcl.2011.10.104
54582865 124277 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770959 124277 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
54584825 124308 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770990 124308 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
25130912 371925 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL505061 371925 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
54584825 124308 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL1770990 124308 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
58227157 234852 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354815 234852 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
58227200 235976 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393535 235976 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
58227337 235994 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393553 235994 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
24745335 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 607 14 None 6 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
11957573 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
44595856 180486 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 356 6 4 8 2.3 Nc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375757 180486 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 356 6 4 8 2.3 Nc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
1279 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
4908365 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
CHEMBL129198 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
11957573 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
1250 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
3692 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL19439 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
25129523 370534 40 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL492884 370534 40 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.06.123
1279 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 7960 58 None -3 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
11066922 43275 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129436 43275 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573458 157329 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047447 157329 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573459 157330 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047448 157330 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
9860842 157331 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)cc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047449 157331 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)cc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
11957573 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
1250 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
3692 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL19439 4107 26 None -7 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
71525681 180557 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 180557 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
136042270 142161 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938979 142161 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
135350653 443317 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 6 1 6 2.6 CCCc1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
CHEMBL5938969 443317 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 6 1 6 2.6 CCCc1cc(S(C)(=O)=O)ccc1N(CC)c1ccnc(N)n1 nan
135353297 445020 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 6 2.5 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CC1 nan
CHEMBL5956735 445020 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 332 5 1 6 2.5 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C1CC1 nan
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
25178552 347508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452848 347508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178552 347508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL452848 347508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
90645158 221672 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 334 3 1 7 1.5 COc1ccc(Cl)cc1-c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2014.06.032
CHEMBL3290585 221672 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 334 3 1 7 1.5 COc1ccc(Cl)cc1-c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2014.06.032
57399828 140598 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 345 5 1 5 3.8 CC(C)(C)CCNc1cc(N2CCN(C3CCCCC3)CC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916502 140598 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 345 5 1 5 3.8 CC(C)(C)CCNc1cc(N2CCN(C3CCCCC3)CC2)ncn1 10.1016/j.bmcl.2011.07.114
805994 348407 6 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL455133 348407 6 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm800876b
805994 348407 6 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL455133 348407 6 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm901379s
168286141 385469 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 385469 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
46890167 21578 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN1CCC(N(C)CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
CHEMBL1085872 21578 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN1CCC(N(C)CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
9966927 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128252 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1007/s00044-004-0106-7
9966927 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL128252 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0341047
9966927 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL128252 42734 3 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
12686479 317316 1 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1021/jm7014217
CHEMBL414183 317316 1 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1021/jm7014217
1265 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
6422124 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
CHEMBL14638 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
1265 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
6422124 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
CHEMBL14638 1941 37 None -2290 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
57390262 140456 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 290 1 2 7 1.2 Nc1nc(N2CC(N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915050 140456 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 290 1 2 7 1.2 Nc1nc(N2CC(N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
155552102 350528 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 3 3 5 1.0 CC(C)(C)CNc1nccc(N2CCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597352 350528 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 3 3 5 1.0 CC(C)(C)CNc1nccc(N2CCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
25178936 370045 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489060 370045 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178936 370045 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489060 370045 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
137646103 313791 0 None None None Human 7.2 pKi = 7.2 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 393 8 3 3 3.7 O=C(O)C(Cc1cccc2ccccc12)NC(=O)[C@@H](CS)Cc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4084275 313791 0 None None None Human 7.2 pKi = 7.2 Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 393 8 3 3 3.7 O=C(O)C(Cc1cccc2ccccc12)NC(=O)[C@@H](CS)Cc1ccccc1 10.1016/j.ejmech.2016.09.074
137395068 463622 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 382 6 2 6 3.2 Nc1nccc(N(Cc2cc[nH]n2)c2ccc(F)cc2OCC(F)(F)F)n1 nan
CHEMBL6051449 463622 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 382 6 2 6 3.2 Nc1nccc(N(Cc2cc[nH]n2)c2ccc(F)cc2OCC(F)(F)F)n1 nan
42624149 219680 0 None -2 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 219680 0 None -2 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
135353301 431237 0 None None None Human 6.2 pKi = 6.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 410 6 1 8 2.9 CS(=O)(=O)c1ccc(N(Cc2ccncn2)c2ccnc(N)n2)c(C2CCC2)c1 nan
CHEMBL5915583 431237 0 None None None Human 6.2 pKi = 6.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 410 6 1 8 2.9 CS(=O)(=O)c1ccc(N(Cc2ccncn2)c2ccnc(N)n2)c(C2CCC2)c1 nan
58227127 235984 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393543 235984 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
1247 7944 80 None -74 11 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -74 11 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -74 11 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -74 11 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
44395308 139115 0 None 39 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 369 1 1 2 2.2 CN1CCN(C(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186108 139115 0 None 39 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 369 1 1 2 2.2 CN1CCN(C(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
155552061 350445 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 350445 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10017821 213508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 213508 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1247 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 7944 80 None -12 11 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10023327 333639 0 None -144 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 333639 0 None -144 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11499454 156096 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 6 2 2 2.5 CC(C)(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL202638 156096 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 6 2 2 2.5 CC(C)(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
10446240 156666 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
CHEMBL203263 156666 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
11622495 158229 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206303 158229 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
1267 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
3035905 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
CHEMBL260374 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
12686479 317316 1 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL414183 317316 1 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1016/j.bmcl.2011.06.123
25129523 370534 40 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 370534 40 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
25129527 370651 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL493720 370651 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
70681962 157349 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.3 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047467 157349 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.3 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCNCC1 10.1016/j.ejmech.2012.06.016
70688339 157350 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047468 157350 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1267 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
3035905 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
CHEMBL260374 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
1267 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
1267 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
3035905 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
3035905 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
CHEMBL260374 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
CHEMBL260374 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
24854635 196688 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 310 1 0 4 3.0 Cc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL261519 196688 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 310 1 0 4 3.0 Cc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
10085528 389937 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 288 7 3 3 2.8 N=C(NCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL550570 389937 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 288 7 3 3 2.8 N=C(NCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10041484 390012 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 316 9 3 3 3.6 N=C(NCCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL551047 390012 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 316 9 3 3 3.6 N=C(NCCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1267 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -28 9 Human 7.2 pKi = 7.2 Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1252 4121 15 None -79 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
9793868 4121 15 None -79 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL417096 4121 15 None -79 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
71681641 180493 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 350 8 4 8 2.2 CC(C)CCc1cc(NCCNc2cc(Cl)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375764 180493 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 350 8 4 8 2.2 CC(C)CCc1cc(NCCNc2cc(Cl)nc(N)n2)nc(N)n1 10.1021/jm301886t
11492189 157665 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 8 1 2 2.5 CCN(CC)CCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205511 157665 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 209 8 1 2 2.5 CCN(CC)CCCCCc1c[nH]cn1 10.1021/jm0504353
14712103 124637 5 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 201 5 2 2 1.7 c1ccc(CNCCc2c[nH]cn2)cc1 10.1016/j.bmcl.2011.06.123
CHEMBL17740 124637 5 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 201 5 2 2 1.7 c1ccc(CNCCc2c[nH]cn2)cc1 10.1016/j.bmcl.2011.06.123
12741697 196513 2 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL260565 196513 2 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.06.123
9793921 137428 5 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 164 2 1 1 2.5 c1nc(CC2CCCCC2)c[nH]1 10.1016/j.bmcl.2011.06.123
CHEMBL1824228 137428 5 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 164 2 1 1 2.5 c1nc(CC2CCCCC2)c[nH]1 10.1016/j.bmcl.2011.06.123
24764570 157326 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 2 2 2 1.9 CN[C@@H]1CCN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047444 157326 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 2 2 2 1.9 CN[C@@H]1CCN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
25178938 370023 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm901379s
CHEMBL488885 370023 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm901379s
933006 274003 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2c(c1)[nH]c1c(N3CCN(C)CC3)ncnc12 10.1039/C5MD00022J
CHEMBL3739430 274003 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2c(c1)[nH]c1c(N3CCN(C)CC3)ncnc12 10.1039/C5MD00022J
10419556 19694 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106913 19694 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
168273549 385346 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 385346 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
66572103 157300 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cnccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047261 157300 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cnccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
164627020 369677 0 None -144 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 369677 0 None -144 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
10515993 20291 0 None -27 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 267 9 2 3 3.0 CCCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079918 20291 0 None -27 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 267 9 2 3 3.0 CCCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
54587792 124312 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.2 Nc1nc(N2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770994 124312 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.2 Nc1nc(N2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1016/j.bmcl.2011.03.017
90645156 221670 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 313 3 1 7 0.9 CN1CCN(c2nc(N)nc(-c3ccc(N(C)C)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290583 221670 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 313 3 1 7 0.9 CN1CCN(c2nc(N)nc(-c3ccc(N(C)C)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
763018 274163 9 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 6 1.3 Cc1nnc2c(N3CCN(C)CC3)nc3ccccc3n12 10.1039/C5MD00022J
CHEMBL3740846 274163 9 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 6 1.3 Cc1nnc2c(N3CCN(C)CC3)nc3ccccc3n12 10.1039/C5MD00022J
44414498 161457 0 None -173 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 7 0 2 6.9 CN(Cc1ccc(-c2ccc(CN(C)C3CCCCC3)cc2)cc1)C1CCCCC1 10.1016/j.bmc.2008.10.029
CHEMBL212775 161457 0 None -173 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 7 0 2 6.9 CN(Cc1ccc(-c2ccc(CN(C)C3CCCCC3)cc2)cc1)C1CCCCC1 10.1016/j.bmc.2008.10.029
44414433 276842 0 None -8 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 352 13 2 2 5.9 CCCCCNCc1ccc(-c2ccc(CNCCCCC)cc2)cc1 10.1016/j.bmc.2008.10.029
CHEMBL379545 276842 0 None -8 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 352 13 2 2 5.9 CCCCCNCc1ccc(-c2ccc(CNCCCCC)cc2)cc1 10.1016/j.bmc.2008.10.029
10419556 19694 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106913 19694 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
164623155 368864 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 352 3 4 4 3.4 N/C(=N\C(=O)Nc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4863393 368864 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 352 3 4 4 3.4 N/C(=N\C(=O)Nc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
57395260 141977 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1ccc2nc(N)nc(N3CCN(C)CC3)c2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935563 141977 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1ccc2nc(N)nc(N3CCN(C)CC3)c2c1 10.1016/j.bmcl.2011.10.104
135350562 407139 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 389 7 1 6 3.1 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)N(C)CC)cc1C1CCC1 nan
CHEMBL5762573 407139 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 389 7 1 6 3.1 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)N(C)CC)cc1C1CCC1 nan
135350569 451309 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 5 1 6 3.1 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(CC)c1ccnc(N)n1 nan
CHEMBL6024478 451309 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 374 5 1 6 3.1 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(CC)c1ccnc(N)n1 nan
11408069 175236 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
CHEMBL221211 175236 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
11408069 175236 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL221211 175236 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
24825995 140416 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914795 140416 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
135350675 447064 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 311 5 2 5 2.7 C/C=C/c1cc(C(N)=O)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5979510 447064 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 311 5 2 5 2.7 C/C=C/c1cc(C(N)=O)ccc1N(c1ccnc(N)n1)C(C)C nan
1267 8287 36 None -16 9 Mouse 7.2 pKi = 7.2 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -16 9 Mouse 7.2 pKi = 7.2 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -16 9 Mouse 7.2 pKi = 7.2 Binding
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
762810 444117 11 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 262 2 0 5 2.0 CCc1cc2c(N3CCN(C)CC3)ncnc2s1 10.1016/j.bmc.2009.08.059
CHEMBL594730 444117 11 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 262 2 0 5 2.0 CCc1cc2c(N3CCN(C)CC3)ncnc2s1 10.1016/j.bmc.2009.08.059
51354299 121672 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 247 8 1 4 2.4 CCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688945 121672 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 247 8 1 4 2.4 CCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
136773074 313265 0 None None None Human 5.2 pKi = 5.2 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4077914 313265 0 None None None Human 5.2 pKi = 5.2 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
57400473 141975 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 361 3 1 6 2.8 CC(=O)c1cccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935561 141975 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 361 3 1 6 2.8 CC(=O)c1cccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)c1 10.1016/j.bmcl.2011.10.104
57397301 140152 0 None -67 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910382 140152 0 None -67 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
127026018 274895 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753985 274895 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
73346048 182664 0 None -15 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 307 7 2 3 3.0 O=C(NCCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL2413359 182664 0 None -15 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 307 7 2 3 3.0 O=C(NCCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164617783 367899 0 None -104 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 367899 0 None -104 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
71519499 177369 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 2 1 6 2.1 CN1CCN(c2nc(N)nc3c2cc(-c2ccc(F)cc2)n3C)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314768 177369 0 None None None Human 4.2 pKi = 4.2 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 340 2 1 6 2.1 CN1CCN(c2nc(N)nc3c2cc(-c2ccc(F)cc2)n3C)CC1 10.1016/j.bmcl.2012.10.139
58227196 413549 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 207 3 2 5 0.4 CC(C)Nc1nccc(N2CC(N)C2)n1 nan
CHEMBL5830987 413549 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 207 3 2 5 0.4 CC(C)Nc1nccc(N2CC(N)C2)n1 nan
135350844 411262 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 325 5 2 5 3.0 CC(C)N(c1ccnc(N)n1)c1ccc(C(N)=O)cc1C1CCC1 nan
CHEMBL5805642 411262 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 325 5 2 5 3.0 CC(C)N(c1ccnc(N)n1)c1ccc(C(N)=O)cc1C1CCC1 nan
58227388 235979 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 nan
CHEMBL3393538 235979 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 nan
54583872 124278 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770960 124278 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)n2)C1 10.1016/j.bmcl.2011.03.017
1279 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
4908365 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
CHEMBL129198 7960 58 None -3 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
58227388 235979 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393538 235979 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
155517880 350627 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
155517880 350627 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 350627 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
46890626 20918 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@@H]3CCCN[C@@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083097 20918 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@@H]3CCCN[C@@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
25178938 370023 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm800876b
CHEMBL488885 370023 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm800876b
9812843 470101 1 None -4 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78838 470101 1 None -4 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL4748908 478366 0 None -7 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 297 5 1 5 1.9 CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
647957 62735 11 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 2 0 6 0.4 Cc1cc(N2CCN(C)CC2)nc(N2CCOCC2)n1 10.1039/C5MD00022J
CHEMBL1381010 62735 11 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 2 0 6 0.4 Cc1cc(N2CCN(C)CC2)nc(N2CCOCC2)n1 10.1039/C5MD00022J
747187 274068 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 249 4 1 3 2.8 Cc1cc2nc(SCCN(C)C)[nH]c2cc1C 10.1039/C5MD00022J
CHEMBL3739949 274068 6 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 249 4 1 3 2.8 Cc1cc2nc(SCCN(C)C)[nH]c2cc1C 10.1039/C5MD00022J
168268716 385305 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 385305 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168268853 385329 0 None -1071 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 385329 0 None -1071 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
5013 200406 24 None -16 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 227 1 0 3 2.0 CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL288591 200406 24 None -16 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 227 1 0 3 2.0 CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm7014217
10243990 20225 0 None -79 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.6 CCCCC(C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079552 20225 0 None -79 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.6 CCCCC(C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
11065080 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1007/s00044-004-0106-7
CHEMBL129488 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1007/s00044-004-0106-7
135353322 410673 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 368 4 1 4 5.6 Cc1cc(S(F)(F)(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5799137 410673 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 368 4 1 4 5.6 Cc1cc(S(F)(F)(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
135353307 413812 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 288 5 1 4 3.7 CCCc1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5833671 413812 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 288 5 1 4 3.7 CCCc1cc(F)ccc1N(c1ccnc(N)n1)C(C)C nan
135350556 427965 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 336 4 1 4 4.7 C/C=C/c1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5882115 427965 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 336 4 1 4 4.7 C/C=C/c1cc(C(F)(F)F)ccc1N(c1ccnc(N)n1)C(C)C nan
135353281 450167 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 423 5 1 6 5.8 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cscn1)c1ccnc(N)n1 nan
CHEMBL6012332 450167 0 None None None Human 8.2 pKi = 8.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 423 5 1 6 5.8 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cscn1)c1ccnc(N)n1 nan
11065080 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0341047
CHEMBL129488 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0341047
117724523 235970 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393529 235970 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
11594278 38594 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL120591 38594 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
11065080 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL129488 43286 1 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
44462956 19931 0 None -2 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL1077276 19931 0 None -2 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
71603140 180548 0 None 97 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 3 2 5 1.5 CNC1CN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376794 180548 0 None 97 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 3 2 5 1.5 CNC1CN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
25147772 347506 9 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 347506 9 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25147772 347506 9 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL452847 347506 9 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
44129131 431167 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 440 8 1 7 2.1 CCN(CC)S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591500 431167 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 440 8 1 7 2.1 CCN(CC)S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
25071319 372221 16 None 9 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 372221 16 None 9 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
16082828 155180 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213886 155180 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
57398091 140379 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 3.0 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914757 140379 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 3.0 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
57401517 140396 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)c(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914774 140396 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)c(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
3035746 371399 6 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL498770 371399 6 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/jm7014777
136030655 119281 0 None 2 3 Mouse 8.1 pKi = 8.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 119281 0 None 2 3 Mouse 8.1 pKi = 8.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136192874 119282 0 None 1 3 Mouse 8.1 pKi = 8.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 119282 0 None 1 3 Mouse 8.1 pKi = 8.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1247 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
1375 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
774 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL90 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
1247 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
53321919 119278 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 119278 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10060213 202962 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 202962 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155491015 350461 6 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 350461 6 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
44609412 180503 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 322 6 4 8 1.6 Nc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375773 180503 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 322 6 4 8 1.6 Nc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
25129523 370534 40 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm301886t
CHEMBL492884 370534 40 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm301886t
51354584 121684 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 6 1 4 2.4 c1nc(CCCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688976 121684 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 6 1 4 2.4 c1nc(CCCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
76314798 215736 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 314 3 1 7 1.4 CN1CCN(c2cc(-c3ccc([N+](=O)[O-])cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL3133131 215736 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 314 3 1 7 1.4 CN1CCN(c2cc(-c3ccc([N+](=O)[O-])cc3)nc(N)n2)CC1 10.1039/C2MD20212C
136042269 142160 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938978 142160 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
71525678 180554 0 None -6 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 180554 0 None -6 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25178937 370047 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL489062 370047 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25071319 372221 16 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 372221 16 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44129209 465540 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 586 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccc(I)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL608373 465540 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 586 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccc(I)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11013044 42769 2 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 333 4 1 2 3.2 O=C(c1cc2ccccc2[nH]1)N1CCN(CCc2ccccc2)CC1 10.1021/jm0341047
CHEMBL128470 42769 2 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 333 4 1 2 3.2 O=C(c1cc2ccccc2[nH]1)N1CCN(CCc2ccccc2)CC1 10.1021/jm0341047
122194625 252070 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
CHEMBL3629828 252070 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
52952957 125879 0 None -29 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789799 125879 0 None -29 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL4748908 478366 0 None -7 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 297 5 1 5 1.9 CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
24854703 331697 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 364 5 0 6 3.0 COc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL428606 331697 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 364 5 0 6 3.0 COc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL4748908 478366 0 None -7 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 297 5 1 5 1.9 CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
156013005 351447 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 899 20 2 7 10.6 Cc1cc(OCCCNC(=O)CCCCCN2/C(=C\C=C\C=C\C3=[N+](CCCCS(=O)(=O)[O-])c4ccccc4C3(C)C)C(C)(C)c3ccccc32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4639472 351447 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 899 20 2 7 10.6 Cc1cc(OCCCNC(=O)CCCCCN2/C(=C\C=C\C=C\C3=[N+](CCCCS(=O)(=O)[O-])c4ccccc4C3(C)C)C(C)(C)c3ccccc32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
168268827 385323 0 None -30 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 385323 0 None -30 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
52952957 125879 0 None -29 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789799 125879 0 None -29 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
135353294 410481 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 5 1 6 2.6 CCc1cc(S(C)(=O)=O)ccc1N(c1ccnc(N)n1)C(C)C nan
CHEMBL5796949 410481 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 5 1 6 2.6 CCc1cc(S(C)(=O)=O)ccc1N(c1ccnc(N)n1)C(C)C nan
135353321 450324 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 409 7 1 8 2.9 CCc1cc(S(=O)(=O)C(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6014069 450324 0 None None None Human 7.2 pKi = 7.2 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 409 7 1 8 2.9 CCc1cc(S(=O)(=O)C(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
25071319 372221 16 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 372221 16 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
46228101 443435 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594022 443435 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL4748908 478366 0 None -7 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 297 5 1 5 1.9 CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
46228083 433208 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 374 5 2 6 3.1 CN1CCN(c2cc(NCc3ccc(-c4ccccc4)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593551 433208 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 374 5 2 6 3.1 CN1CCN(c2cc(NCc3ccc(-c4ccccc4)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
135353366 428153 0 None None None Human 6.1 pKi = 6.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 350 7 1 7 1.8 CCc1cc(S(C)(=O)=O)ccc1N(CCOC)c1ccnc(N)n1 nan
CHEMBL5884291 428153 0 None None None Human 6.1 pKi = 6.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 350 7 1 7 1.8 CCc1cc(S(C)(=O)=O)ccc1N(CCOC)c1ccnc(N)n1 nan
46890549 20915 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083085 20915 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
112936352 274897 0 None -17 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754008 274897 0 None -17 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
155563489 349337 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 3 1 6 0.7 CCC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4573929 349337 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 3 1 6 0.7 CCC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71518865 177339 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 333 2 2 6 1.8 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(C#N)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314494 177339 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 333 2 2 6 1.8 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(C#N)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
57401167 142115 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938846 142115 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
24826679 140373 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2cccc(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914751 140373 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2cccc(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
168294161 385551 0 None -38 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 385551 0 None -38 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
168294770 385565 0 None -31 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 385565 0 None -31 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
44450438 196475 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc3ccccc3nc2NCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260371 196475 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc3ccccc3nc2NCc2ccccc2)CC1 10.1021/jm7014217
71528209 177848 1 None -1148 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 177848 1 None -1148 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
121238069 314979 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting methodDisplacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4097856 314979 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting methodDisplacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
135353286 425627 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 345 6 1 7 3.4 CCOc1cc(F)ccc1N(Cc1cncs1)c1ccnc(N)n1 nan
CHEMBL5855998 425627 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 345 6 1 7 3.4 CCOc1cc(F)ccc1N(Cc1cncs1)c1ccnc(N)n1 nan
24826268 140323 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 3 2 6 2.8 CCN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914544 140323 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 3 2 6 2.8 CCN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
56851443 143856 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 356 7 2 3 4.6 c1ccc(CN/C(=N/C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963459 143856 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 356 7 2 3 4.6 c1ccc(CN/C(=N/C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
121238069 314979 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4097856 314979 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.09.035
25178132 370196 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL490073 370196 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25178132 370196 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL490073 370196 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
168283321 385439 0 None -30 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 385439 0 None -30 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
24759622 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL443764 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm800876b
24759622 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm7014217
24759622 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL443764 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL443764 334248 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm901379s
164622259 369017 0 None -7244 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4865965 369017 0 None -7244 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
24826167 140417 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914796 140417 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
54581938 124290 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770972 124290 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
46890019 21632 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086085 21632 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
24994945 219679 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 207 2 2 5 0.2 CN[C@@H]1CCN(c2cc(C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236567 219679 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 207 2 2 5 0.2 CN[C@@H]1CCN(c2cc(C)nc(N)n2)C1 10.1021/jm401727m
1223 1963 35 None -21 8 Human 7.1 pKi = 7.1 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 1963 35 None -21 8 Human 7.1 pKi = 7.1 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 1963 35 None -21 8 Human 7.1 pKi = 7.1 Binding
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
51354301 121676 0 None -10 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 121676 0 None -10 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
164609017 367735 0 None -13 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 367735 0 None -13 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
168294166 385559 0 None -16 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 385559 0 None -16 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
168294178 385579 0 None -25 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 385579 0 None -25 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
127026019 274863 0 None -6 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753705 274863 0 None -6 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
11546127 195851 1 None None None Human 5.1 pKi = 5.1 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL25725 195851 1 None None None Human 5.1 pKi = 5.1 Binding
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
10715823 20261 0 None -20 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 281 10 2 3 3.3 CCCCC(CC)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079747 20261 0 None -20 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 281 10 2 3 3.3 CCCCC(CC)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
1267 8287 36 None -28 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 8287 36 None -28 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 8287 36 None -28 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
25109291 366002 9 None -478 12 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1016/j.bmcl.2011.06.123
CHEMBL519240 366002 9 None -478 12 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1016/j.bmcl.2011.06.123
25071319 372221 16 None -9 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.06.123
CHEMBL509540 372221 16 None -9 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.06.123
1247 7944 80 None -199 11 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 7944 80 None -199 11 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 7944 80 None -199 11 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 7944 80 None -199 11 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10446295 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
1277 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL185951 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
1267 8287 36 None -16 9 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 8287 36 None -16 9 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 8287 36 None -16 9 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
937120 349122 4 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 244 1 0 3 1.8 CN1CCN(C(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2020.115924
CHEMBL4568949 349122 4 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 244 1 0 3 1.8 CN1CCN(C(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2020.115924
71681974 180478 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1cc(-c2ccccc2)nc(N)n1)c1ccnc(N)n1 10.1021/jm301886t
CHEMBL2375749 180478 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1cc(-c2ccccc2)nc(N)n1)c1ccnc(N)n1 10.1021/jm301886t
71681475 180484 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 317 8 5 9 1.0 CC(C)CNc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375755 180484 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 317 8 5 9 1.0 CC(C)CNc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681643 180495 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375766 180495 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 378 9 4 8 3.1 CC(C)CNc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
71681645 180497 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
CHEMBL2375768 180497 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
11679993 157676 0 None -25 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205559 157676 0 None -25 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
11087453 157309 1 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047270 157309 1 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572113 157314 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3ccc(N)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047275 157314 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3ccc(N)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573457 157328 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 283 2 1 2 2.4 Cc1cccc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047446 157328 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 283 2 1 2 2.4 Cc1cccc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
70688340 157358 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3c(F)ccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047476 157358 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3c(F)ccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
51354875 121692 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 1 4 2.8 c1nc(CCCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688986 121692 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 1 4 2.8 c1nc(CCCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25178937 370047 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL489062 370047 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
11846635 160196 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
CHEMBL211242 160196 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
4060730 43234 34 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 43234 34 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
90645159 221673 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 338 2 1 6 2.2 CN1CCN(c2nc(N)nc(-c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290586 221673 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 338 2 1 6 2.2 CN1CCN(c2nc(N)nc(-c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
162671115 366321 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 266 2 0 3 1.9 CN1CCN(CC2Cc3cc(Cl)ccc3O2)CC1 10.1016/j.bmc.2020.115924
CHEMBL4792753 366321 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 266 2 0 3 1.9 CN1CCN(CC2Cc3cc(Cl)ccc3O2)CC1 10.1016/j.bmc.2020.115924
10197870 19637 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106612 19637 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
91613 41853 21 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 41853 21 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
71681474 180483 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 246 5 4 8 -0.0 Nc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
CHEMBL2375754 180483 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 246 5 4 8 -0.0 Nc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
11637064 156622 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203228 156622 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
11708125 158173 2 None -251 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206000 158173 2 None -251 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
11499376 275869 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 5 2 2 2.1 CC(C)(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL377491 275869 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 195 5 2 2 2.1 CC(C)(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
56672434 137424 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 1 2 3.3 CN1CCC(=Cc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL1824048 137424 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 1 2 3.3 CN1CCC(=Cc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2011.06.123
66572109 157306 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3c([N+](=O)[O-])cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047267 157306 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3c([N+](=O)[O-])cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10957150 157323 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047441 157323 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
3939214 254615 3 None -1 2 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 262 1 1 1 3.4 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1 10.1016/j.bmcl.2004.08.035
CHEMBL365257 254615 3 None -1 2 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 262 1 1 1 3.4 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1 10.1016/j.bmcl.2004.08.035
11086114 21714 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL108649 21714 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
2247 1042 63 None -87 37 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
249 1042 63 None -87 37 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
2603 1042 63 None -87 37 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
CHEMBL296419 1042 63 None -87 37 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
DB00637 1042 63 None -87 37 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
44417471 27036 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 175 4 5 3 -0.5 N=C(N)NCCCSC(=N)N 10.1021/jm060880d
CHEMBL1187948 27036 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 175 4 5 3 -0.5 N=C(N)NCCCSC(=N)N 10.1021/jm060880d
164614841 368571 0 None -223 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4858849 368571 0 None -223 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
9923162 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128613 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
10967174 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129540 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1007/s00044-004-0106-7
135353326 405786 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 421 6 1 6 5.6 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5748892 405786 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 421 6 1 6 5.6 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353303 409342 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 390 4 1 5 4.3 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1OC(F)(F)F nan
CHEMBL5784858 409342 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 390 4 1 5 4.3 CC(C)N(c1ccnc(N)n1)c1ccc(Br)cc1OC(F)(F)F nan
135353313 452161 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 400 5 1 6 3.8 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(F)(F)F)cc1C1CCC1 nan
CHEMBL6033426 452161 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 400 5 1 6 3.8 CCN(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(F)(F)F)cc1C1CCC1 nan
1247 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
9923162 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128613 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0341047
10967174 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
1279 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
54580746 124151 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.1 Nc1nc(N2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770160 124151 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.1 Nc1nc(N2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2011.03.017
1279 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
4908365 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL129198 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
58227157 234852 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354815 234852 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
58227179 235989 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393548 235989 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
58227259 235997 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 235997 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1279 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 7960 58 None -3 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
42624150 219689 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236577 219689 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
24827129 140406 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2c(Cl)cc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914785 140406 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2c(Cl)cc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
9923162 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128613 42797 10 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
10967174 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129540 43294 1 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
44129212 431165 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.3 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(C(F)(F)F)cccc3n2)CC1 10.1021/jm901379s
CHEMBL591496 431165 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.3 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(C(F)(F)F)cccc3n2)CC1 10.1021/jm901379s
24825522 370877 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
CHEMBL494982 370877 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
51354300 121673 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688946 121673 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
23650961 8371 34 None None None Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C 10.1016/j.ejmech.2023.115151
9276 8371 34 None None None Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C 10.1016/j.ejmech.2023.115151
CHEMBL3301609 8371 34 None None None Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C 10.1016/j.ejmech.2023.115151
DB12522 8371 34 None None None Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C 10.1016/j.ejmech.2023.115151
58227373 350473 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 350473 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
168294182 385590 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 385590 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
46890546 20845 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082771 20845 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
135353296 431220 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 438 6 1 8 3.0 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ncccn1)c1ccnc(N)n1 nan
CHEMBL5915411 431220 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 438 6 1 8 3.0 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(Cc1ncccn1)c1ccnc(N)n1 nan
46228069 445627 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 323 3 1 7 1.2 CN1CCN(c2nc(N)nc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596348 445627 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 323 3 1 7 1.2 CN1CCN(c2nc(N)nc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
63868172 350029 1 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 222 2 1 6 -0.2 CCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4590628 350029 1 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 222 2 1 6 -0.2 CCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
164614549 368249 0 None -575 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 368249 0 None -575 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164621681 368869 0 None -64 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863523 368869 0 None -64 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
164627241 369698 0 None -269 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4876267 369698 0 None -269 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
11086114 21714 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL108649 21714 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
71519347 177366 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 274 4 2 6 1.2 CCCCn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314765 177366 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 274 4 2 6 1.2 CCCCn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
54754351 140488 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915535 140488 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
54754351 140488 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915535 140488 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
58227242 235993 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2cnnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393552 235993 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2cnnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
121238067 331909 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.09.035
CHEMBL4290148 331909 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.09.035
57400778 140481 0 None 199 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915346 140481 0 None 199 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
54584827 124314 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770996 124314 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
57400778 140481 0 None 199 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915346 140481 0 None 199 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400589 142154 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)cnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938972 142154 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)cnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
90645164 221678 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1C 10.1016/j.ejmech.2014.06.032
CHEMBL3290591 221678 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1C 10.1016/j.ejmech.2014.06.032
57399016 140447 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915040 140447 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
135350861 443374 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 5 1 6 2.7 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C(C)C nan
CHEMBL5939594 443374 0 None None None Human 7.1 pKi = 7.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 5 1 6 2.7 CCN(c1ccnc(N)n1)c1ccc(S(C)(=O)=O)cc1C(C)C nan
46890548 20914 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083084 20914 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46929551 40628 0 None -52 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243335 40628 0 None -52 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
5159263 24670 10 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 259 4 3 4 0.8 Cc1cc(C)nc(N/C(N)=N/CCc2c[nH]cn2)n1 10.1021/jm7014777
CHEMBL1162351 24670 10 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 259 4 3 4 0.8 Cc1cc(C)nc(N/C(N)=N/CCc2c[nH]cn2)n1 10.1021/jm7014777
71525679 180555 0 None -9 6 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 180555 0 None -9 6 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25178130 372858 1 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL515870 372858 1 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
25178130 372858 1 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL515870 372858 1 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
164622153 368857 0 None -181 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863347 368857 0 None -181 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
54581939 124302 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770984 124302 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
122193095 251968 0 None -3 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assayDisplacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628042 251968 0 None -3 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assayDisplacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
58227260 235987 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393546 235987 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
57398176 140599 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 273 2 0 5 1.4 CN1CCN(c2cc(N3[C@@H]4CCC[C@@H]3C4)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916503 140599 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 273 2 0 5 1.4 CN1CCN(c2cc(N3[C@@H]4CCC[C@@H]3C4)ncn2)CC1 10.1016/j.bmcl.2011.07.114
127050776 277535 0 None 6 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805437 277535 0 None 6 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
164627189 369592 0 None -831 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 369592 0 None -831 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
71519015 177345 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 246 1 2 5 0.7 CN1CCCN(c2nc(N)nc3[nH]ccc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314500 177345 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 246 1 2 5 0.7 CN1CCCN(c2nc(N)nc3[nH]ccc23)CC1 10.1016/j.bmcl.2012.10.139
57400737 140449 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Cl)ccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915042 140449 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Cl)ccc3c2n1 10.1016/j.bmcl.2011.08.014
57395494 140443 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915032 140443 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
57395499 140452 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 2 7 1.8 C[C@H]1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CCN1 10.1016/j.bmcl.2011.08.014
CHEMBL1915046 140452 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 2 7 1.8 C[C@H]1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CCN1 10.1016/j.bmcl.2011.08.014
46890677 21611 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086038 21611 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
56851612 143829 0 None -19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 398 9 2 3 5.3 CCCCN/C(=N/Cc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963245 143829 0 None -19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 398 9 2 3 5.3 CCCCN/C(=N/Cc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm201042n
56851602 143831 0 None -18 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 364 9 2 3 4.7 CCCCN/C(=N/Cc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963260 143831 0 None -18 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 364 9 2 3 4.7 CCCCN/C(=N/Cc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1021/jm201042n
25178345 347543 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccco3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452925 347543 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccco3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354303 121679 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.7 c1nc(CCCn2cc(C3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688971 121679 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 259 5 1 4 2.7 c1nc(CCCn2cc(C3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25147771 348296 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454890 348296 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10656971 40309 3 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL123137 40309 3 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1021/jm7014217
25179123 372258 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL510181 372258 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
10197870 19637 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106612 19637 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
168273471 385344 0 None -1862 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 385344 0 None -1862 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
57402472 140151 0 None -1258 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910381 140151 0 None -1258 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44576985 24669 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 212 4 7 4 -1.3 CC(/C=C(\C)NNC(=N)N)=N/NC(=N)N 10.1021/jm7014777
CHEMBL1162347 24669 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 212 4 7 4 -1.3 CC(/C=C(\C)NNC(=N)N)=N/NC(=N)N 10.1021/jm7014777
71519010 177340 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 386 2 2 5 2.7 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Br)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314495 177340 0 None None None Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 386 2 2 5 2.7 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Br)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
135353342 408747 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 420 6 2 5 5.3 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ccn[nH]1)c1ccnc(N)n1 nan
CHEMBL5778709 408747 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 420 6 2 5 5.3 CCc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ccn[nH]1)c1ccnc(N)n1 nan
135353344 429592 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 363 5 1 6 4.0 CCc1cc(C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL5899196 429592 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 363 5 1 6 4.0 CCc1cc(C(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
135353329 462711 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 405 6 1 7 4.6 Nc1nccc(N(Cc2cocn2)c2ccc(OC(F)(F)F)cc2C2CCC2)n1 nan
CHEMBL6042655 462711 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 405 6 1 7 4.6 Nc1nccc(N(Cc2cocn2)c2ccc(OC(F)(F)F)cc2C2CCC2)n1 nan
135353330 464528 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 421 5 1 6 5.7 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncoc1C)c1ccnc(N)n1 nan
CHEMBL6060897 464528 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 421 5 1 6 5.7 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1ncoc1C)c1ccnc(N)n1 nan
135353284 464587 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6061715 464587 0 None None None Human 8.1 pKi = 8.1 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 407 5 1 6 5.4 Cc1cc(S(F)(F)(F)(F)F)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
1247 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
1375 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
774 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
CHEMBL90 7944 80 None -12 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
54587790 124298 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770980 124298 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
54753437 140454 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2014.12.027
CHEMBL1915048 140454 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2014.12.027
11750684 174463 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
CHEMBL219982 174463 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
54753437 140454 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1021/jm401727m
CHEMBL1915048 140454 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1021/jm401727m
24825794 140328 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914549 140328 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
71525679 180555 0 None 9 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 180555 0 None 9 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25071940 370596 0 None 5 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 370596 0 None 5 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
71525586 180553 0 None 22 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 2 1 6 0.9 CCc1cnc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376799 180553 0 None 22 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 272 2 1 6 0.9 CCc1cnc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
44129135 430933 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 454 6 1 8 1.1 CN1CCN(c2nc(NCCS(=O)(=O)N3CCOCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591250 430933 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 454 6 1 8 1.1 CN1CCN(c2nc(NCCS(=O)(=O)N3CCOCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
53378711 219690 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236578 219690 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
54753437 140454 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915048 140454 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
135525668 140483 0 None 263 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915348 140483 0 None 263 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
49841611 141981 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 347 2 1 5 3.2 Cc1cccc(C)c1-c1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935567 141981 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 347 2 1 5 3.2 Cc1cccc(C)c1-c1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
1248 2933 20 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
3077 2933 20 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
90045 2933 20 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
CHEMBL12344 2933 20 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
11615753 145147 6 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3sccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL200546 145147 6 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3sccc3[nH]2)CC1 10.1021/jm0502081
10444761 251897 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3ccsc3[nH]2)CC1 10.1021/jm0502081
CHEMBL362495 251897 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3ccsc3[nH]2)CC1 10.1021/jm0502081
16082826 161769 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@H]2C[C@@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214156 161769 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@H]2C[C@@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
122193097 251970 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628044 251970 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
57390344 140492 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 248 5 3 6 0.3 CNC1CN(c2cc(N)nc(NCC3CC3)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915539 140492 0 None None None Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 248 5 3 6 0.3 CNC1CN(c2cc(N)nc(NCC3CC3)n2)C1 10.1016/j.bmcl.2011.07.125
135350851 427653 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 337 4 1 6 3.4 CC(C)N(c1ccnc(N)n1)c1ccc(C#N)cc1OC(F)(F)F nan
CHEMBL5878684 427653 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 337 4 1 6 3.4 CC(C)N(c1ccnc(N)n1)c1ccc(C#N)cc1OC(F)(F)F nan
49841607 141969 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
CHEMBL1935555 141969 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 257 1 1 5 1.3 Cc1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
12686451 469002 2 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 1 0 4 2.0 CN1CCN(c2cnc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
CHEMBL6992 469002 2 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 1 0 4 2.0 CN1CCN(c2cnc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
44546969 428137 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 5 2 4 1.7 CCCCNc1cc(N2CCNCC2)ccn1 nan
CHEMBL5884129 428137 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).Binding Assay: Cell pellets from SK-N-MC cells stably or transiently transfected with human H4 receptor (NCBI accession No. AF312230) were used for the binding assays. Cell pellets were homogenized in 50 mM Tris/5 mM EDTA buffer and supernatants from an 800 g spin were collected and recentrifuged at 30,000 g for 30 min. Pellets were rehomogenized in 50 mM Tris/5 mM EDTA buffer. For competition binding studies, cell membranes were incubated with 2x KD (10 nM),[3H] histamine (Specific activity: 14.2 to 23 Ci/mmol), with or without test compounds for 45 to 60 min at 4 to 25° C. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108).
ChEMBL 234 5 2 4 1.7 CCCCNc1cc(N2CCNCC2)ccn1 nan
51354010 121668 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 281 7 1 4 2.6 c1ccc(Cc2cn(CCCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688941 121668 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 281 7 1 4 2.6 c1ccc(Cc2cn(CCCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
127036979 274891 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753962 274891 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
118720434 234846 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 241 3 2 5 0.6 CN[C@@H]1CCN(c2cc(CCl)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354808 234846 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 241 3 2 5 0.6 CN[C@@H]1CCN(c2cc(CCl)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
11212855 175205 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL220934 175205 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
57401602 140600 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 242 1 0 4 1.3 Cc1ccc(C#N)c(N2CC3CN(C)CC3C2)n1 10.1016/j.bmcl.2011.07.114
CHEMBL1916504 140600 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 242 1 0 4 1.3 Cc1ccc(C#N)c(N2CC3CN(C)CC3C2)n1 10.1016/j.bmcl.2011.07.114
156010537 352224 0 None -69 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 430 11 2 3 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCNCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4651053 352224 0 None -69 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 430 11 2 3 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCNCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
90654503 219848 0 None -123 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238447 219848 0 None -123 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
57394626 140589 0 None 14 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916494 140589 0 None 14 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
49841723 141974 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 349 3 1 6 2.6 COc1ccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)cc1 10.1016/j.bmcl.2011.10.104
CHEMBL1935560 141974 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 349 3 1 6 2.6 COc1ccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)cc1 10.1016/j.bmcl.2011.10.104
112936251 274671 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 274671 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
25178340 370048 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm800876b
CHEMBL489069 370048 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm800876b
25179123 372258 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL510181 372258 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25178340 370048 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm901379s
CHEMBL489069 370048 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm901379s
164618690 369433 0 None -13 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872375 369433 0 None -13 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
135353359 406339 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 7 1 7 2.7 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(CCOC)c1ccnc(N)n1 nan
CHEMBL5754114 406339 0 None None None Human 7.0 pKi = 7.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 404 7 1 7 2.7 CCc1cc(S(=O)(=O)C(F)(F)F)ccc1N(CCOC)c1ccnc(N)n1 nan
44547126 235968 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393527 235968 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
118725540 235965 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 1.9 CN[C@@H]1CCN(c2ccnc(N3CCCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393524 235965 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 1.9 CN[C@@H]1CCN(c2ccnc(N3CCCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
46890676 21563 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 1 4 4.0 Cc1cc(OCCCN2CC3CN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1085804 21563 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 1 4 4.0 Cc1cc(OCCCN2CC3CN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57393651 142153 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3cc4cccnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938971 142153 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3cc4cccnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
24853666 312042 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 1 1 4 1.7 CN1CCCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL406327 312042 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 292 1 1 4 1.7 CN1CCCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
112936267 274699 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752383 274699 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
127051301 277488 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 277488 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25130914 370502 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL492677 370502 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
71519178 177362 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.9 Nc1nc(N2CC[C@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314761 177362 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 312 2 3 5 1.9 Nc1nc(N2CC[C@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
135350841 411492 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 402 5 1 6 3.8 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(C)C)cc1C(F)(F)F nan
CHEMBL5808209 411492 0 None None None Human 6.0 pKi = 6.0 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 402 5 1 6 3.8 CC(C)N(c1ccnc(N)n1)c1ccc(S(=O)(=O)C(C)C)cc1C(F)(F)F nan
135350550 451831 0 None None None Human 7.0 pKi = 7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 6 1 7 3.2 CCCc1cc(C#N)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
CHEMBL6030126 451831 0 None None None Human 7.0 pKi = 7 Binding
Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.Binding Assay on Recombinant Human Histamine H4 Receptor: Receptor binding was assessed using isolated plasma membranes from SKNMC neuroblastoma cell lines stably expressing recombinant human H4 receptor. To isolate plasma membrane enriched in recombinant human H4 receptor, cells were collected from 100 culture dishes (150 mm) in PBS-EDTA. The cells were pellet by centrifugation (800 g) and resuspended in 5×TE buffer (50 mM Tris/5 mM EDTA). The cells were then homogenized and centrifuged at 1000 g for 10 min. The supernatant was collected and centrifuged for an additional 26000 g for 30 min. The supernatant was removed and the pellet was gently resuspended in 30 ml of 5×TE buffer. Protein concentration was then determined using Bradford protein assay (Bradford, M. M., Anal. Biochem., 1976, 72: 248-254). Isolated cell membranes were incubated with 2×KD (10 nM), [3H] histamine (Specific activity: 23 Ci/mmol), with or without test compounds for 45 min at 25° C. Nonspecific binding was defined with 100 μM cold histamine. Ki values were calculated based on an experimentally determined appropriate KD values according to Cheng and Prusoff (Biochem. Pharmacol. 1973, 22(23):3099-3108). Membranes were harvested by rapid filtration using the 96 well Brandel system or a cell harvester using a Whatman GF/C filter or filter plates treated with 0.5% polyethylenimine (PEI), and washed 4 times with ice-cold 50 mM Tris/5 mM EDTA buffer. Filters were then dried, mixed with scintillant and radioactive counts were determined.
ChEMBL 334 6 1 7 3.2 CCCc1cc(C#N)ccc1N(Cc1cocn1)c1ccnc(N)n1 nan
127052293 277526 5 None 34 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 277526 5 None 34 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1530 4450 49 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 4450 49 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 4450 49 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 4450 49 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 4450 49 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
124087 2860 75 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 2860 75 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 2860 75 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 2860 75 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 2860 75 None None None Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
71548412 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
9879 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
CHEMBL4790724 3905 26 None None None Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
71548412 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
9879 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
CHEMBL4790724 3905 26 None None None Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
1279 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
4908365 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
CHEMBL129198 7960 58 None 177 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1247 7944 80 None -81 9 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 7944 80 None -81 9 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 7944 80 None -81 9 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 7944 80 None -81 9 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1237 7956 17 None -99 3 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
156615 7956 17 None -99 3 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
CHEMBL268229 7956 17 None -99 3 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1247 7944 80 None -25 9 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 7944 80 None -25 9 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 7944 80 None -25 9 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 7944 80 None -25 9 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1220 8031 0 None -17 2 Human 7.5 pKd None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 7 0 4 2.7 COc1ccc(cc1)CN(c1ccc(cn1)[3H])CCN(C)C 11179435
656400 8031 0 None -17 2 Human 7.5 pKd None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 7 0 4 2.7 COc1ccc(cc1)CN(c1ccc(cn1)[3H])CCN(C)C 11179435
CHEMBL1628641 8031 0 None -17 2 Human 7.5 pKd None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 7 0 4 2.7 COc1ccc(cc1)CN(c1ccc(cn1)[3H])CCN(C)C 11179435
1241 4169 46 None -19 3 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
3614 4169 46 None -19 3 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
CHEMBL507 4169 46 None -19 3 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1275 7601 0 None None None Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 7944 80 None -6 9 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
10660 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1224 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
441281 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL1200406 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB00985 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB13636 2953 69 None -77 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
115237 118408 70 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4137 118408 70 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 118408 70 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 118408 70 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2247 1042 63 None -87 37 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 1042 63 None -87 37 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 1042 63 None -87 37 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 1042 63 None -87 37 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 1042 63 None -87 37 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
5625 432667 52 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
799 432667 52 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
CHEMBL593 432667 52 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
DB00705 432667 52 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
1613 4786 46 None -28 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 4786 46 None -28 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 4786 46 None -28 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 4786 46 None -28 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 4786 46 None -28 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
16106 236970 34 None -23 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2111 236970 34 None -23 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 236970 34 None -23 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2132 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
4761 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
667440 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL1193 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL376103 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
DB01620 27696 28 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
135398737 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2818 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL253391 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 1973 61 None -54 61 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 8289 46 None -2 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 8289 46 None -2 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 8289 46 None -2 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 8289 46 None -2 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 8289 46 None -2 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
16362 6358 55 None -81 22 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 6358 55 None -81 22 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 6358 55 None -81 22 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 6358 55 None -81 22 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 6358 55 None -81 22 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135398737 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2818 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL253391 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 1973 61 None -44 61 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
103 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2782 65627 47 None None None Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
672 65627 47 None None None Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
CHEMBL1407943 65627 47 None None None Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
DB15932 65627 47 None None None Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
1210 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
5281070 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
90475904 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1200927 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB09555 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 1893 53 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2286 6468 43 None -7 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 6468 43 None -7 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 6468 43 None -7 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 6468 43 None -7 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 6468 43 None -7 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2726 1895 54 None -3 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 1895 54 None -3 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 1895 54 None -3 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 1895 54 None -3 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 1895 54 None -3 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1204 3953 0 None -3 12 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 3953 0 None -3 12 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 3953 0 None -3 12 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 3953 0 None -3 12 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 3953 0 None -3 12 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 3953 0 None -5 12 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 3953 0 None -5 12 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 3953 0 None -5 12 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 3953 0 None -5 12 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 3953 0 None -5 12 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 3953 0 None -1 12 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 3953 0 None -1 12 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 3953 0 None -1 12 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 3953 0 None -1 12 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
180 829 44 None -6 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 829 44 None -6 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 829 44 None -6 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 829 44 None -6 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 829 44 None -6 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
277 2680 45 None -15 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 2680 45 None -15 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 2680 45 None -15 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 2680 45 None -15 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 2680 45 None -15 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1204 3953 0 None -1 12 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 3953 0 None -1 12 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 3953 0 None -1 12 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 3953 0 None -1 12 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 3953 0 None -1 12 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
135398737 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2818 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL253391 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 1973 61 None -57 61 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
23650961 8371 34 None None None Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
9276 8371 34 None None None Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
CHEMBL3301609 8371 34 None None None Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
DB12522 8371 34 None None None Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
1265 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
1265 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
1265 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
6422124 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
6422124 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
6422124 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
CHEMBL14638 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
CHEMBL14638 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
CHEMBL14638 1941 37 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
1267 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
3035905 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
CHEMBL260374 8287 36 None -28 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
10446295 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
1277 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
CHEMBL185951 4352 37 None 263 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
1223 1963 35 None -154 8 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 1963 35 None -154 8 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 1963 35 None -154 8 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1274 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
3063228 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
CHEMBL1196470 8815 10 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
1269 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
1269 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
37463 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
37463 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
CHEMBL275443 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
CHEMBL275443 249 35 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
1223 1963 35 None -165 8 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 1963 35 None -165 8 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 1963 35 None -165 8 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1223 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
1223 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
1223 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1223 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
1223 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
2790 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
2790 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
2790 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
2790 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
CHEMBL14690 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
CHEMBL14690 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
CHEMBL14690 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
CHEMBL14690 1963 35 None -21 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
24994634 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
8984 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
CHEMBL3236549 4374 36 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
45257132 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
8983 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
CHEMBL595180 7480 22 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
1278 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1278 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
1278 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
4908365 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
4908365 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
4908365 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
CHEMBL129198 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
CHEMBL129198 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
CHEMBL129198 4390 0 None None None Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
117072554 4133 0 None 81 4 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
8982 4133 0 None 81 4 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
24745335 607 14 None 6 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
8985 607 14 None 6 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
CHEMBL1915540 607 14 None 6 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
DB15027 607 14 None 6 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
5048 6373 55 None -81283 10 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
8924 6373 55 None -81283 10 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
9948102 6373 55 None -81283 10 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
CHEMBL462605 6373 55 None -81283 10 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
DB11642 6373 55 None -81283 10 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
441082 2406 38 None -2137 7 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
8981 2406 38 None -2137 7 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
CHEMBL191703 2406 38 None -2137 7 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
11697697 5180 30 None -4570 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
7346 5180 30 None -4570 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
CHEMBL476323 5180 30 None -4570 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
DB11910 5180 30 None -4570 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
1547484 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
2761 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 1937 56 None -1 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
10058807 4123 2 None None None Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
1276 4123 2 None None None Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
CHEMBL2261340 4123 2 None None None Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
135398737 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
2818 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL253391 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 1973 61 None -54 61 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
1238 4258 10 None -35 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
6603865 4258 10 None -35 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
CHEMBL11919 4258 10 None -35 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
1248 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
1248 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
1248 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
1248 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
3077 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
3077 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
3077 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
3077 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
90045 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
90045 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
90045 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
90045 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
CHEMBL12344 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
CHEMBL12344 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
CHEMBL12344 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
CHEMBL12344 2933 20 None -7 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
135398737 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
2818 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL253391 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 1973 61 None -44 61 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
11313837 5081 11 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
1254 5081 11 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
CHEMBL175782 5081 11 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
124846 3981 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
1273 3981 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
CHEMBL67601 3981 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
12656 4171 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
1270 4171 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
CHEMBL12704 4171 0 None None None Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
1194 95 1 None 1 2 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
23786499 95 1 None 1 2 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
CHEMBL26116 95 1 None 1 2 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
1229 1532 0 None -19 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 1532 0 None -19 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1229 1532 0 None -15 6 Mouse 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 1532 0 None -15 6 Mouse 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1236 4227 0 None -398 6 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 4227 0 None -398 6 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 4227 0 None -398 6 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1242 4163 0 None -446 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 4163 0 None -446 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 4163 0 None -446 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1268 170 0 None None None Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 15947036
1268 170 0 None None None Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 16432504
92613 170 0 None None None Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 15947036
92613 170 0 None None None Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 16432504
1236 4227 0 None -251 6 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 4227 0 None -251 6 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 4227 0 None -251 6 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
135398737 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
135398737 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
135398737 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
135398737 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
2818 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
2818 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
2818 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
2818 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
38 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
38 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
38 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
722 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
722 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
722 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
CHEMBL253391 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
CHEMBL253391 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
CHEMBL253391 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL253391 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
CHEMBL42 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
CHEMBL42 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
CHEMBL42 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
DB00363 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
DB00363 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
DB00363 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 1973 61 None -57 61 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
1242 4163 0 None -281 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 4163 0 None -281 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 4163 0 None -281 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1236 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1236 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
1236 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
1236 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
156615 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
156615 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
156615 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
CHEMBL268229 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
CHEMBL268229 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
CHEMBL268229 4227 0 None -125 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1271 4161 0 None None None Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
44292270 4161 0 None None None Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
CHEMBL46296 4161 0 None None None Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
1239 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
1239 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
3614 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
3614 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
912 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
912 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
CHEMBL268490 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
CHEMBL268490 4155 0 None -100 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
1229 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179434
1229 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179436
1229 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11181941
1229 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1229 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 15947036
5311293 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179434
5311293 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179436
5311293 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11181941
5311293 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 1532 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 15947036
1204 3953 0 None -5 12 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 3953 0 None -5 12 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 3953 0 None -5 12 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 3953 0 None -5 12 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 3953 0 None -5 12 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 3953 0 None -3 12 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 3953 0 None -3 12 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 3953 0 None -3 12 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 3953 0 None -3 12 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 3953 0 None -3 12 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1242 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1242 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1242 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
3614 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
3614 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
CHEMBL507 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
CHEMBL507 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 4163 0 None -31 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
1267 8287 36 None -16 9 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1267 8287 36 None -11 9 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 8287 36 None -16 9 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 8287 36 None -11 9 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 8287 36 None -16 9 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 8287 36 None -11 9 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1266 4207 0 None -17 3 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 9 3 4 2.8 N[C@H](SCCCc1cnc[nH]1)NCCc1ccc(cc1)I 11179436
5311186 4207 0 None -17 3 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 9 3 4 2.8 N[C@H](SCCCc1cnc[nH]1)NCCc1ccc(cc1)I 11179436
1226 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
1226 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
41376 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
41376 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
CHEMBL12608 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
CHEMBL12608 4125 18 None 2 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
1251 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
1251 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
1251 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
3035842 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
3035842 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
3035842 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
CHEMBL18661 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
CHEMBL18661 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
CHEMBL18661 4115 26 None -120 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1204 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1375 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
774 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
CHEMBL90 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
DB05381 3953 0 None -1 12 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
11957573 4107 26 None -14 7 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
11957573 4107 26 None -14 7 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 4107 26 None -14 7 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 4107 26 None -14 7 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 4107 26 None -14 7 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 4107 26 None -14 7 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 4107 26 None -14 7 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 4107 26 None -14 7 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
11957573 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
11957573 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
11957573 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
11957573 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
1250 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
1250 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
1250 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
3692 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
3692 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
3692 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
CHEMBL19439 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
CHEMBL19439 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
CHEMBL19439 4107 26 None -7 7 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071