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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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
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13103 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
171037436 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
CHEMBL5395893 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
13103 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
171037436 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
CHEMBL5395893 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 10.1021/acs.jmedchem.3c00951
127044155 278394 0 None None None Human 10.6 pEC50 = 10.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 223 7 2 3 3.4 CCCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
CHEMBL3827638 278394 0 None None None Human 10.6 pEC50 = 10.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 223 7 2 3 3.4 CCCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
177648470 392091 0 None None None Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5590375 392091 0 None None None Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
54678947 46867 0 None None None Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 209 6 2 3 3.0 CCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
CHEMBL13302 46867 0 None None None Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 209 6 2 3 3.0 CCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
11212 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127045422 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3828298 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11212 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
127045422 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL3828298 337 2 None -9 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
177648470 392091 0 None None None Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5590375 392091 0 None None None Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
11212 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
127045422 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3828298 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
177648470 392091 0 None None None Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5590375 392091 0 None None None Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
11212 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127045422 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3828298 337 2 None -9 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
149547952 391496 0 None None None Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 2 2 3.8 CCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5569898 391496 0 None None None Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 2 2 3.8 CCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
171037982 391251 2 None -5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565525 391251 2 None -5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
171037982 391251 2 None -5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565525 391251 2 None -5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177660496 390761 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 279 11 2 2 4.5 CCCCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5557607 390761 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 279 11 2 2 4.5 CCCCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11212 337 2 None -9 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
127045422 337 2 None -9 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3828298 337 2 None -9 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
54728809 46555 0 None None None Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 265 10 2 3 4.6 CCCCCCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
CHEMBL13276 46555 0 None None None Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 265 10 2 3 4.6 CCCCCCCCCCCc1cc(O)cc(O)n1 10.1021/acs.jmedchem.3c01923
177654897 391585 0 None None None Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571259 391585 0 None None None Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177652736 391265 0 None None None Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 6 2 2 3.0 O=c1cc(O)cc(CCCCCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5565836 391265 0 None None None Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 6 2 2 3.0 O=c1cc(O)cc(CCCCCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
177639275 390587 0 None None None Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 293 12 2 2 4.9 CCCCCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5552972 390587 0 None None None Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 293 12 2 2 4.9 CCCCCCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11211 8982 40 None -16 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None -16 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None -16 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
177648720 392169 0 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5591819 392169 0 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
176155012 391448 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 239 8 2 3 2.8 CCCCCCCCOc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5569090 391448 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 239 8 2 3 2.8 CCCCCCCCOc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11211 8982 40 None -16 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None -16 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None -16 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
171037986 391601 2 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5571529 391601 2 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
171037982 391251 2 None -5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565525 391251 2 None -5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177648720 392169 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5591819 392169 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
54678947 46867 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 209 6 2 3 3.0 CCCCCCCc1cc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL13302 46867 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 209 6 2 3 3.0 CCCCCCCc1cc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177649189 391974 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 225 7 2 3 2.4 CCCCCCCOc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5583983 391974 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 225 7 2 3 2.4 CCCCCCCOc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127044155 278394 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 223 7 2 3 3.4 CCCCCCCCc1cc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827638 278394 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 223 7 2 3 3.4 CCCCCCCCc1cc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
23646340 175291 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
ChEMBL 252 7 2 4 3.1 CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O 10.1021/acs.jmedchem.3c00951
CHEMBL221598 175291 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
ChEMBL 252 7 2 4 3.1 CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O 10.1021/acs.jmedchem.3c00951
23646340 175291 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assayAgonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assay
ChEMBL 252 7 2 4 3.1 CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O 10.1021/acs.jmedchem.0c01378
CHEMBL221598 175291 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assayAgonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assay
ChEMBL 252 7 2 4 3.1 CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O 10.1021/acs.jmedchem.0c01378
177652196 391631 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 5 2 2 2.6 O=c1cc(O)cc(CCCCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5572086 391631 0 None None None Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 5 2 2 2.6 O=c1cc(O)cc(CCCCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
177653890 391558 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5570876 391558 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
177656749 391806 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 299 4 2 3 2.8 O=c1cc(O)cc(CCc2ccc(OC(F)(F)F)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5575107 391806 0 None None None Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 299 4 2 3 2.8 O=c1cc(O)cc(CCc2ccc(OC(F)(F)F)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
172463022 388865 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 289 5 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5426206 388865 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 289 5 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 10.1021/acs.jmedchem.3c00951
133081959 6533 4 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
9871 6533 4 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL4444010 6533 4 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
178310552 467491 0 None None None Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 307 13 1 3 5.6 CCCCCCCCCc1cc(O)cc(OCCCCC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6177124 467491 0 None None None Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 307 13 1 3 5.6 CCCCCCCCCc1cc(O)cc(OCCCCC)n1 10.1021/acs.jmedchem.4c02335
11208 2931 74 None 2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
137656606 315446 0 None None None Human 5.0 pEC50 = 5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 304 3 2 2 4.0 COC(=O)c1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4103279 315446 0 None None None Human 5.0 pEC50 = 5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 304 3 2 2 4.0 COC(=O)c1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
177650335 391948 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 282 3 2 6 1.7 O=c1cc(O)cc(-c2ccc(Oc3cncnc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5583631 391948 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 282 3 2 6 1.7 O=c1cc(O)cc(-c2ccc(Oc3cncnc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
178322553 467040 0 None None None Human 5.0 pEC50 = 5.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 349 12 0 4 5.3 CCCCCCCCCc1cc(OC)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6167167 467040 0 None None None Human 5.0 pEC50 = 5.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 349 12 0 4 5.3 CCCCCCCCCc1cc(OC)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
156500043 466966 0 None None None Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 8 1 5 3.9 CCCc1ccc(CCc2cc(O)cc(OCC3OCC(C)CO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6165391 466966 0 None None None Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 8 1 5 3.9 CCCc1ccc(CCc2cc(O)cc(OCC3OCC(C)CO3)n2)cc1 10.1021/acs.jmedchem.4c02335
3893 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
4642 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
5534 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL108766 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
DB03017 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
10354234 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
3893 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
4642 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
5534 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108766 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
DB03017 4658 74 None -2 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
172454079 388113 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 279 5 0 3 2.6 COc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5410350 388113 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 279 5 0 3 2.6 COc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
127044004 278418 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 7 2 5 3.4 Oc1cc(O)nc(SCCCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827935 278418 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 7 2 5 3.4 Oc1cc(O)nc(SCCCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
172454079 388113 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 279 5 0 3 2.6 COc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5410350 388113 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 279 5 0 3 2.6 COc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
137658184 315583 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.6b01593
CHEMBL4104992 315583 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.6b01593
178309794 467451 0 None None None Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176329 467451 0 None None None Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
127044149 278385 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 7 2 4 2.8 CCCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827580 278385 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 7 2 4 2.8 CCCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
156499873 467238 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 4 5.1 CCCCCCCCCc1cc(O)cc(OCc2cccnc2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6171791 467238 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 4 5.1 CCCCCCCCCc1cc(O)cc(OCc2cccnc2)n1 10.1021/acs.jmedchem.4c02335
178323725 467335 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 11 1 3 5.7 CCCCCCCCCc1cc(O)cc(OCc2ccccc2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6174170 467335 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 11 1 3 5.7 CCCCCCCCCc1cc(O)cc(OCc2ccccc2)n1 10.1021/acs.jmedchem.4c02335
10354234 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
125356668 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
5846 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL3827832 335 45 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
11208 2931 74 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by top-count liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
11208 2931 74 None 2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
153309768 385373 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None None None Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
137635702 311972 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.6b01593
CHEMBL4062512 311972 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.6b01593
127045478 278462 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 368 16 2 5 6.5 CCCCCCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828578 278462 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 368 16 2 5 6.5 CCCCCCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
137632827 312315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 314 2 2 0 5.5 Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4066454 312315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 314 2 2 0 5.5 Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 10.1021/acs.jmedchem.6b01593
11005 5494 74 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
2806 5494 74 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL111077 5494 74 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB08231 5494 74 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
137643701 314156 2 None -2 2 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.01 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.01 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None -2 2 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.01 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.01 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
11213 2971 9 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
154578239 2971 9 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
CHEMBL4743442 2971 9 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
137643701 314156 2 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
CHEMBL4088884 314156 2 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
127043534 278399 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 312 12 2 5 4.9 CCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827684 278399 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 312 12 2 5 4.9 CCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
176155018 391783 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 1 2 3.7 CCCCCCCCCc1cc(OC)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574706 391783 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 1 2 3.7 CCCCCCCCCc1cc(OC)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
177654247 391536 0 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 269 2 2 5 2.1 Cc1nnc(-c2ccc(-c3cc(O)cc(=O)[nH]3)cc2)o1 10.1021/acs.jmedchem.3c01923
CHEMBL5570610 391536 0 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 269 2 2 5 2.1 Cc1nnc(-c2ccc(-c3cc(O)cc(=O)[nH]3)cc2)o1 10.1021/acs.jmedchem.3c01923
11210 6531 3 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
146025748 6531 3 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL4538049 6531 3 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
177652635 391744 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5574017 391744 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177657427 391551 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 8 1 3 3.4 CCCCCCCCCc1cc(O)cc(=O)n1C 10.1021/acs.jmedchem.3c01923
CHEMBL5570744 391551 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 8 1 3 3.4 CCCCCCCCCc1cc(O)cc(=O)n1C 10.1021/acs.jmedchem.3c01923
11213 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
154578239 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
CHEMBL4743442 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
11213 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
154578239 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
CHEMBL4743442 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
177655775 391216 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5564975 391216 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177652635 391744 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5574017 391744 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
127044143 278468 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 210 6 2 4 2.4 CCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828708 278468 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 210 6 2 4 2.4 CCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
172446198 387333 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cccc(CCOc2ccc(Cl)c3ccccc23)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5394311 387333 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cccc(CCOc2ccc(Cl)c3ccccc23)[nH]1 10.1021/acs.jmedchem.3c00951
156499911 467398 0 None None None Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
CHEMBL6175294 467398 0 None None None Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
11211 8982 40 None -6 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None -6 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None -6 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
172446198 387333 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cccc(CCOc2ccc(Cl)c3ccccc23)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5394311 387333 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cccc(CCOc2ccc(Cl)c3ccccc23)[nH]1 10.1021/acs.jmedchem.3c00951
178308271 467116 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 337 11 1 4 3.5 CCCCCCCCCc1cc(OCC2COCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6169002 467116 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 337 11 1 4 3.5 CCCCCCCCCc1cc(OCC2COCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
10354234 335 45 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11208 2931 74 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
5849 138 40 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
97783 138 40 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
CHEMBL4278254 138 40 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
177653890 391558 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5570876 391558 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
177657109 391810 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5575143 391810 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
5850 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting methodAgonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.0c01378
94216 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting methodAgonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.0c01378
CHEMBL4288936 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting methodAgonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.0c01378
172447122 387315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 293 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Br)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5393955 387315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 293 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Br)cc2)c1 10.1021/acs.jmedchem.3c00951
5850 207 53 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
94216 207 53 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4288936 207 53 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
172447122 387315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 293 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Br)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5393955 387315 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 293 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Br)cc2)c1 10.1021/acs.jmedchem.3c00951
11211 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
172453887 388349 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(CCOc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5415128 388349 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(CCOc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
156499952 467346 0 None None None Human 4.9 pEC50 = 4.9 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 370 8 1 5 4.3 CCCc1ccc(CN(C)c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174338 467346 0 None None None Human 4.9 pEC50 = 4.9 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 370 8 1 5 4.3 CCCc1ccc(CN(C)c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
172453887 388349 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(CCOc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5415128 388349 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(CCOc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
176155025 392341 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
CHEMBL5594779 392341 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
176155025 392341 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL5594779 392341 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.4c02335
11211 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
1912564 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3827756 8982 40 None -16 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
177654260 391598 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571478 391598 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177656403 391798 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574940 391798 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
178310753 467373 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 11 1 2 5.2 CCCCCCCCCc1cc(OCc2ccccc2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6174874 467373 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 11 1 2 5.2 CCCCCCCCCc1cc(OCc2ccccc2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
11211 8982 40 None -16 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
1912564 8982 40 None -16 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3827756 8982 40 None -16 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acsmedchemlett.6b00025
178318640 466606 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 305 11 1 2 4.8 CCCCCCCCCc1cc(OCC2CCC2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6150009 466606 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 305 11 1 2 4.8 CCCCCCCCCc1cc(OCC2CCC2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
11005 5494 74 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
2806 5494 74 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL111077 5494 74 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
DB08231 5494 74 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
178309894 467298 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 277 11 1 2 4.2 C=CCOc1cc(CCCCCCCCC)[nH]c(=O)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6173356 467298 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 277 11 1 2 4.2 C=CCOc1cc(CCCCCCCCC)[nH]c(=O)c1 10.1021/acs.jmedchem.4c02335
178323647 467517 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 333 11 1 2 5.6 CCCCCCCCCc1cc(OCC2CCCCC2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6177600 467517 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 333 11 1 2 5.6 CCCCCCCCCc1cc(OCC2CCCCC2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
172456864 388519 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 1 2 2.7 O=c1cccc(CCOc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5418284 388519 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 1 2 2.7 O=c1cccc(CCOc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.3c00951
172458591 388732 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 269 4 0 2 3.0 [O-][n+]1cccc(CCOC2CCCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5422968 388732 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 269 4 0 2 3.0 [O-][n+]1cccc(CCOC2CCCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
172456864 388519 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 1 2 2.7 O=c1cccc(CCOc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5418284 388519 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 1 2 2.7 O=c1cccc(CCOc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.3c00951
172458591 388732 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 269 4 0 2 3.0 [O-][n+]1cccc(CCOC2CCCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5422968 388732 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 269 4 0 2 3.0 [O-][n+]1cccc(CCOC2CCCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
156499964 467461 0 None None None Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 369 8 1 4 4.7 CC(C)Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176562 467461 0 None None None Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 369 8 1 4 4.7 CC(C)Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
171037986 391601 2 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5571529 391601 2 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
177653966 391699 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5573172 391699 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
169561646 389741 0 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
178323130 467425 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 3 4.6 CCCCCCCCCc1cc(OCc2ccccn2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6175922 467425 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 3 4.6 CCCCCCCCCc1cc(OCc2ccccn2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
156500025 467360 0 None None None Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174631 467360 0 None None None Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
16064 327827 56 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4456892 327827 56 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
11211 8982 40 None -16 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None -16 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None -16 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
10354234 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5533 8561 70 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
8180 8561 70 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108030 8561 70 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
140898896 390717 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5556864 390717 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178317703 466849 0 None None None Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 285 5 1 4 3.1 CCCc1cc(O)cc(OCC2Cc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6162518 466849 0 None None None Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 285 5 1 4 3.1 CCCc1cc(O)cc(OCC2Cc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
177656732 391791 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574832 391791 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
176155025 392341 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
CHEMBL5594779 392341 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
10354234 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
125356668 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
5846 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL3827832 335 45 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
172444226 387369 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cc(F)cc(CCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5394821 387369 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cc(F)cc(CCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172444226 387369 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cc(F)cc(CCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5394821 387369 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cc(F)cc(CCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
10171 3702 28 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 5.8 pEC50 = 5.8 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
177642586 392200 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 285 2 2 5 2.1 O=c1cc(O)cc(-c2ccc(OC3=NCCCC3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5592504 392200 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 285 2 2 5 2.1 O=c1cc(O)cc(-c2ccc(OC3=NCCCC3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
5288266 40330 44 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL1232858 40330 44 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
DB02767 40330 44 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
177653890 391558 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5570876 391558 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
137643701 314156 2 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
CHEMBL4088884 314156 2 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
153309768 385373 0 None None None Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None None None Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
11211 8982 40 None -16 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
1912564 8982 40 None -16 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3827756 8982 40 None -16 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
140898896 390717 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5556864 390717 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178310919 467356 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 309 12 1 4 4.5 CCCCCCCCCc1cc(O)cc(OC(C)COC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6174552 467356 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 309 12 1 4 4.5 CCCCCCCCCc1cc(O)cc(OC(C)COC)n1 10.1021/acs.jmedchem.4c02335
178308987 467383 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 333 11 1 3 6.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCC2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6175020 467383 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 333 11 1 3 6.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCC2)n1 10.1021/acs.jmedchem.4c02335
156500000 467164 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 405 8 1 5 4.7 CCCc1ccc(CCc2cc(O)cc(OCC3COc4ccccc4O3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6170239 467164 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 405 8 1 5 4.7 CCCc1ccc(CCc2cc(O)cc(OCC3COc4ccccc4O3)n2)cc1 10.1021/acs.jmedchem.4c02335
137649817 313311 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.6b01593
CHEMBL4078546 313311 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.6b01593
102583156 314776 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4095532 314776 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
10354234 335 45 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
125356668 335 45 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
5846 335 45 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827832 335 45 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
156500013 467404 0 None None None Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175409 467404 0 None None None Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
177655775 391216 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5564975 391216 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
172454954 387975 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 303 4 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c3c2CCCC3)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5407571 387975 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 303 4 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c3c2CCCC3)c1 10.1021/acs.jmedchem.3c00951
172454954 387975 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 303 4 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c3c2CCCC3)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5407571 387975 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 303 4 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c3c2CCCC3)c1 10.1021/acs.jmedchem.3c00951
156499933 466902 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 4 5.1 CCCCCCCCCc1cc(O)cc(OCc2ccccn2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6163757 466902 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 328 11 1 4 5.1 CCCCCCCCCc1cc(O)cc(OCc2ccccn2)n1 10.1021/acs.jmedchem.4c02335
177638762 390450 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 224 7 3 3 2.5 CCCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5542260 390450 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 224 7 3 3 2.5 CCCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
177654897 391585 0 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571259 391585 0 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
133081959 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
9871 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4444010 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
133081959 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
9871 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL4444010 6533 4 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
177645103 392400 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 210 6 3 3 2.1 CCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5595586 392400 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 210 6 3 3 2.1 CCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
177644081 392254 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 3 2 2 3.2 CC(C)(C)c1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5593496 392254 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 271 3 2 2 3.2 CC(C)(C)c1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
11209 3191 70 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
2969 2799 70 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
10171 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
177648720 392169 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5591819 392169 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
79034 389968 61 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 11 2 2 3.0 O=C(O)CCCCCCCCCCCO 10.1039/C7MD00130D
CHEMBL55068 389968 61 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 11 2 2 3.0 O=C(O)CCCCCCCCCCCO 10.1039/C7MD00130D
DB03704 389968 61 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 11 2 2 3.0 O=C(O)CCCCCCCCCCCO 10.1039/C7MD00130D
127044148 278390 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 4 2 4 1.9 CC(C)CCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827606 278390 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 4 2 4 1.9 CC(C)CCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
11211 8982 40 None -16 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None -16 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None -16 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
171037982 391251 2 None -5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565525 391251 2 None -5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
156499976 466942 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 321 11 1 4 4.6 CCCCCCCCCc1cc(O)cc(OCC2CCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6164628 466942 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 321 11 1 4 4.6 CCCCCCCCCc1cc(O)cc(OCC2CCCO2)n1 10.1021/acs.jmedchem.4c02335
177653177 391618 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 286 6 3 3 1.8 O=C(NCCCCc1cc(O)cc(=O)[nH]1)c1ccccc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571841 391618 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 286 6 3 3 1.8 O=C(NCCCCc1cc(O)cc(=O)[nH]1)c1ccccc1 10.1021/acs.jmedchem.3c01923
127045479 278465 0 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 210 4 2 5 1.4 C#CCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828642 278465 0 None None None Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 210 4 2 5 1.4 C#CCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177655145 391433 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 258 5 3 3 2.6 CCCc1ccc(CNc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5568831 391433 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 258 5 3 3 2.6 CCCc1ccc(CNc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
172465331 389243 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(OCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5435149 389243 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(OCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
172465331 389243 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(OCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5435149 389243 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 249 4 0 2 2.6 [O-][n+]1cccc(OCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
10171 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
172469537 389319 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cc(CCOc2ccc(Cl)c3ccccc23)cc[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5436803 389319 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cc(CCOc2ccc(Cl)c3ccccc23)cc[nH]1 10.1021/acs.jmedchem.3c00951
172469537 389319 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cc(CCOc2ccc(Cl)c3ccccc23)cc[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL5436803 389319 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 299 4 1 2 3.8 O=c1cc(CCOc2ccc(Cl)c3ccccc23)cc[nH]1 10.1021/acs.jmedchem.3c00951
156499901 466788 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.6 CCCc1ccc(CCc2cc(O)cc(COC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6161204 466788 0 None None None Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.6 CCCc1ccc(CCc2cc(O)cc(COC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
10171 3702 28 None None None Human 6.7 pEC50 = 6.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 6.7 pEC50 = 6.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 6.7 pEC50 = 6.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 6.7 pEC50 = 6.7 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
176155049 391703 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 221 8 1 1 3.7 CCCCCCCCCc1cc(=O)cc[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5573222 391703 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 221 8 1 1 3.7 CCCCCCCCCc1cc(=O)cc[nH]1 10.1021/acs.jmedchem.3c01923
177655957 391721 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5573446 391721 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
177656403 391798 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574940 391798 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
156499906 467331 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2cccc(C(F)(F)F)c2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6174115 467331 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2cccc(C(F)(F)F)c2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
127043533 278407 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 242 7 2 5 3.0 CCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827763 278407 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 242 7 2 5 3.0 CCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
172471663 389448 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5439839 389448 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
177651205 390356 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 236 8 2 2 3.3 CCCCCCCCCc1cc(N)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5532132 390356 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 236 8 2 2 3.3 CCCCCCCCCc1cc(N)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
172471663 389448 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5439839 389448 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
177652708 391178 0 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 252 7 3 3 1.3 CCCC(=O)NCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5564536 391178 0 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 252 7 3 3 1.3 CCCC(=O)NCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
178322293 466913 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 335 11 1 3 4.6 CCCCCCCCCc1cc(OCC2CCCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6164013 466913 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 335 11 1 3 4.6 CCCCCCCCCc1cc(OCC2CCCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
172464049 388953 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.2 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5428112 388953 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.2 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1Cl 10.1021/acs.jmedchem.3c00951
177654260 391598 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571478 391598 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
172464049 388953 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.2 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5428112 388953 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.2 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1Cl 10.1021/acs.jmedchem.3c00951
660705 82233 33 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 214 5 2 5 2.2 CCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL1466478 82233 33 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 214 5 2 5 2.2 CCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
140898896 390717 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5556864 390717 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
2969 2799 70 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
172461860 389078 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 2 3.1 [O-][n+]1cccc(CCOc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5431514 389078 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 2 3.1 [O-][n+]1cccc(CCOc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
11208 2931 74 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
172461860 389078 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 2 3.1 [O-][n+]1cccc(CCOc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5431514 389078 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 2 3.1 [O-][n+]1cccc(CCOc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172449686 388171 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 295 5 0 3 3.1 COc1ccc(OCCc2ccc[n+]([O-])c2)c2ccccc12 10.1021/acs.jmedchem.3c00951
CHEMBL5411553 388171 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 295 5 0 3 3.1 COc1ccc(OCCc2ccc[n+]([O-])c2)c2ccccc12 10.1021/acs.jmedchem.3c00951
172462970 389172 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 1 3.6 [O-][n+]1cccc(CCCc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5433568 389172 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 1 3.6 [O-][n+]1cccc(CCCc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172449686 388171 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 295 5 0 3 3.1 COc1ccc(OCCc2ccc[n+]([O-])c2)c2ccccc12 10.1021/acs.jmedchem.3c00951
CHEMBL5411553 388171 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 295 5 0 3 3.1 COc1ccc(OCCc2ccc[n+]([O-])c2)c2ccccc12 10.1021/acs.jmedchem.3c00951
172462970 389172 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 1 3.6 [O-][n+]1cccc(CCCc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5433568 389172 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 263 4 0 1 3.6 [O-][n+]1cccc(CCCc2cccc3ccccc23)c1 10.1021/acs.jmedchem.3c00951
127045477 278397 0 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 340 14 2 5 5.7 CCCCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827657 278397 0 None None None Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 340 14 2 5 5.7 CCCCCCCCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177655775 391216 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5564975 391216 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
11211 8982 40 None -6 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None -6 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None -6 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
156499885 466963 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.4 CCCc1ccc(COCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6165269 466963 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.4 CCCc1ccc(COCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
156499851 467333 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174163 467333 0 None None None Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
171037986 391601 2 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5571529 391601 2 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
177655775 391216 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5564975 391216 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 257 5 2 2 3.5 CCCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
13413723 278410 4 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 256 8 2 5 3.3 CCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827862 278410 4 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 256 8 2 5 3.3 CCCCCCCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
137649231 313045 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4075099 313045 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
137643701 314156 2 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
11211 8982 40 None -16 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
1912564 8982 40 None -16 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3827756 8982 40 None -16 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127044463 278346 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 262 4 2 5 2.7 CCc1ccc(CSc2nc(O)cc(O)n2)cc1 10.1021/acsmedchemlett.6b00025
CHEMBL3827038 278346 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 262 4 2 5 2.7 CCc1ccc(CSc2nc(O)cc(O)n2)cc1 10.1021/acsmedchemlett.6b00025
172460977 388848 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 267 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Cl)c(F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5425765 388848 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 267 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Cl)c(F)c2)c1 10.1021/acs.jmedchem.3c00951
172460977 388848 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 267 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Cl)c(F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5425765 388848 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 267 4 0 2 2.7 [O-][n+]1cccc(CCOc2ccc(Cl)c(F)c2)c1 10.1021/acs.jmedchem.3c00951
172460369 388551 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 343 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Br)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5419003 388551 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 343 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Br)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172460369 388551 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 343 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Br)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5419003 388551 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 343 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Br)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
11211 8982 40 None -16 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None -16 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None -16 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
178318408 466652 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 325 13 1 5 4.1 CCCCCCCCCc1cc(O)cc(OCC(OC)OC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6151079 466652 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 325 13 1 5 4.1 CCCCCCCCCc1cc(O)cc(OCC(OC)OC)n1 10.1021/acs.jmedchem.4c02335
153309768 385373 0 None None None Human 4.6 pEC50 = 4.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None None None Human 4.6 pEC50 = 4.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
137643701 314156 2 None 2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
CHEMBL4088884 314156 2 None 2 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at GPR84 in mouse bone-marrow-derived neutrophils assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
11208 2931 74 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None 2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
10171 3702 28 None None None Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
137643701 314156 2 None 2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
CHEMBL4088884 314156 2 None 2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
127044150 278423 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 238 7 2 4 3.4 CCCCCCCC(C)c1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828004 278423 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 238 7 2 4 3.4 CCCCCCCC(C)c1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177656258 391548 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.6 CCCc1ccc(COc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5570704 391548 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.6 CCCc1ccc(COc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177651726 390447 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 238 8 3 3 2.9 CCCCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5542189 390447 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 238 8 3 3 2.9 CCCCCCCCNc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
156499869 467252 0 None None None Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172099 467252 0 None None None Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
177654897 391585 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571259 391585 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178309761 467408 0 None None None Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 6 1 4 3.8 Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6175479 467408 0 None None None Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 327 6 1 4 3.8 Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
177654260 391598 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571478 391598 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
11211 8982 40 None -6 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None -6 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None -6 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
2969 2799 70 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
172470062 389399 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 255 4 0 2 2.6 [O-][n+]1cccc(CCOC2CCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5438602 389399 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 255 4 0 2 2.6 [O-][n+]1cccc(CCOC2CCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
177660002 390508 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 272 5 2 3 2.7 CCCc1ccc(CN(C)c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5542968 390508 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 272 5 2 3 2.7 CCCc1ccc(CN(C)c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178311311 467441 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 295 12 1 4 4.1 CCCCCCCCCc1cc(O)cc(OCCOC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6176184 467441 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 295 12 1 4 4.1 CCCCCCCCCc1cc(O)cc(OCCOC)n1 10.1021/acs.jmedchem.4c02335
172470062 389399 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 255 4 0 2 2.6 [O-][n+]1cccc(CCOC2CCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5438602 389399 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 255 4 0 2 2.6 [O-][n+]1cccc(CCOC2CCc3ccccc32)c1 10.1021/acs.jmedchem.3c00951
26612 205 63 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
5848 205 63 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4448230 205 63 None None None Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
172458761 388470 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 247 4 0 1 3.1 [O-][n+]1cccc(CCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5417376 388470 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 247 4 0 1 3.1 [O-][n+]1cccc(CCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
177638978 390552 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 312 5 2 4 1.7 O=C1c2ccccc2C(=O)N1CCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5549817 390552 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 312 5 2 4 1.7 O=C1c2ccccc2C(=O)N1CCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
172459947 388506 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2Cl)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5418045 388506 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2Cl)c1 10.1021/acs.jmedchem.3c00951
172458761 388470 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 247 4 0 1 3.1 [O-][n+]1cccc(CCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5417376 388470 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 247 4 0 1 3.1 [O-][n+]1cccc(CCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
172459947 388506 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2Cl)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5418045 388506 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.9 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2Cl)c1 10.1021/acs.jmedchem.3c00951
137658671 315290 0 None 7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4101219 315290 0 None 7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
11213 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
154578239 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
CHEMBL4743442 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production incubated for 30 mins by luminescence based DiscoverX HitHunter cAMP assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c00951
11213 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.0c01378
154578239 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.0c01378
CHEMBL4743442 2971 9 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.0c01378
177653966 391699 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5573172 391699 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178307603 466952 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 363 17 1 3 7.2 CCCCCCCCCOc1cc(O)cc(CCCCCCCCC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6164905 466952 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 363 17 1 3 7.2 CCCCCCCCCOc1cc(O)cc(CCCCCCCCC)n1 10.1021/acs.jmedchem.4c02335
177655957 391721 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5573446 391721 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
178323080 467386 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 307 13 1 2 5.2 CCCCCCCCCc1cc(OCCCCC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6175044 467386 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 307 13 1 2 5.2 CCCCCCCCCc1cc(OCCCCC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
10354234 335 45 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assayAgonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
10201214 193994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 402 2 2 0 5.8 Brc1ccc2[nH]cc(Cc3c[nH]c4ccc(Br)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL246504 193994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 402 2 2 0 5.8 Brc1ccc2[nH]cc(Cc3c[nH]c4ccc(Br)cc34)c2c1 10.1021/acs.jmedchem.6b01593
10171 3702 28 None None None Human 6.5 pEC50 = 6.5 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 6.5 pEC50 = 6.5 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 6.5 pEC50 = 6.5 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 6.5 pEC50 = 6.5 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
137643701 314156 2 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
172462081 388872 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 3.4 [O-][n+]1cccc(CCOc2ccc(Cl)c(Br)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5426349 388872 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 3.4 [O-][n+]1cccc(CCOc2ccc(Cl)c(Br)c2)c1 10.1021/acs.jmedchem.3c00951
172462081 388872 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 3.4 [O-][n+]1cccc(CCOc2ccc(Cl)c(Br)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5426349 388872 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 3.4 [O-][n+]1cccc(CCOc2ccc(Cl)c(Br)c2)c1 10.1021/acs.jmedchem.3c00951
9944370 193930 3 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL246298 193930 3 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.6b01593
70233802 278431 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 182 4 2 4 1.6 CCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828115 278431 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 182 4 2 4 1.6 CCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
172468371 389223 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 5 0 2 4.1 [O-][n+]1cccc(CCCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5434775 389223 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 5 0 2 4.1 [O-][n+]1cccc(CCCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172468371 389223 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 5 0 2 4.1 [O-][n+]1cccc(CCCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5434775 389223 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 5 0 2 4.1 [O-][n+]1cccc(CCCOc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
153309768 385373 0 None None None Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None None None Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 300 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
137654126 314868 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)c(F)c34)c2c1F 10.1021/acs.jmedchem.6b01593
CHEMBL4096571 314868 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)c(F)c34)c2c1F 10.1021/acs.jmedchem.6b01593
177653890 391558 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5570876 391558 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 255 4 2 2 3.1 O=c1cc(O)cc(-c2ccc(CCC3CC3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
5282900 42009 11 None None None Human 4.4 pEC50 = 4.4 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCC(O)CCC(=O)O 10.1039/C7MD00130D
CHEMBL1269402 42009 11 None None None Human 4.4 pEC50 = 4.4 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCC(O)CCC(=O)O 10.1039/C7MD00130D
127043463 278364 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 248 4 2 5 2.2 Oc1cc(O)nc(SCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827283 278364 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 248 4 2 5 2.2 Oc1cc(O)nc(SCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
1563 145124 51 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL2004471 145124 51 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
169561646 389741 0 None None None Human 4.4 pEC50 = 4.4 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 4.4 pEC50 = 4.4 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
177654897 391585 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571259 391585 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 271 6 2 2 3.2 CCCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
177652537 391626 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1cccc(CCc2cc(O)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.3c01923
CHEMBL5572024 391626 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1cccc(CCc2cc(O)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.3c01923
172451703 388255 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 4.4 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c(C)[n+]1[O-] 10.1021/acs.jmedchem.3c00951
CHEMBL5413298 388255 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 4.4 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c(C)[n+]1[O-] 10.1021/acs.jmedchem.3c00951
172451703 388255 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 4.4 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c(C)[n+]1[O-] 10.1021/acs.jmedchem.3c00951
CHEMBL5413298 388255 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 4 0 2 4.4 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c(C)[n+]1[O-] 10.1021/acs.jmedchem.3c00951
172471462 389439 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 257 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1C 10.1021/acs.jmedchem.3c00951
CHEMBL5439662 389439 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 257 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1C 10.1021/acs.jmedchem.3c00951
177639486 390473 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 245 5 2 3 2.1 O=c1cc(O)cc(CCCOc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5542526 390473 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 245 5 2 3 2.1 O=c1cc(O)cc(CCCOc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
177648720 392169 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5591819 392169 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
177655108 391255 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 4 2 2 2.4 CCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565593 391255 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 243 4 2 2 2.4 CCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
10717 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
44349321 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL124977 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
172471462 389439 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 257 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1C 10.1021/acs.jmedchem.3c00951
CHEMBL5439662 389439 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 257 4 0 2 2.9 Cc1cc(OCCc2ccc[n+]([O-])c2)cc(C)c1C 10.1021/acs.jmedchem.3c00951
137643701 314156 2 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
172471903 389489 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 1 3.6 [O-][n+]1cccc(CCC(F)c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5440770 389489 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 1 3.6 [O-][n+]1cccc(CCC(F)c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
172471903 389489 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 1 3.6 [O-][n+]1cccc(CCC(F)c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5440770 389489 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 265 4 0 1 3.6 [O-][n+]1cccc(CCC(F)c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
11209 3191 70 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
177652768 391439 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2cccc(-c3ccccc3)c2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5568948 391439 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2cccc(-c3ccccc3)c2)[nH]1 10.1021/acs.jmedchem.3c01923
11208 2931 74 None -2 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.0c01378
3071 2931 74 None -2 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.0c01378
CHEMBL446452 2931 74 None -2 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.0c01378
DB11875 2931 74 None -2 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.0c01378
127045482 278414 0 None None None Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 212 3 2 5 1.8 Oc1cc(O)nc(SCC2CCC2)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827914 278414 0 None None None Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 212 3 2 5 1.8 Oc1cc(O)nc(SCC2CCC2)n1 10.1021/acsmedchemlett.6b00025
127045103 278368 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 6 2 5 3.0 Oc1cc(O)nc(SCCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827310 278368 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 6 2 5 3.0 Oc1cc(O)nc(SCCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
10354234 335 45 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
125356668 335 45 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
5846 335 45 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3827832 335 45 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
177653966 391699 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5573172 391699 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
2969 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.3c00951
5532 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.3c00951
CHEMBL107498 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.3c00951
DB03600 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human GPR84 expressed in CHO cells assessed as inhibition of forskolin induced cAMP production pretreated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.3c00951
2969 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 minsAgonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
5532 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 minsAgonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL107498 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 minsAgonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
DB03600 2799 70 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 minsAgonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
23042624 278419 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 5 2 4 2.0 CCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827946 278419 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 5 2 4 2.0 CCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177654260 391598 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5571478 391598 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.9 CCCCOc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
2969 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
2969 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
141409856 391441 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 215 3 2 2 1.9 O=c1cc(O)cc(CCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5568958 391441 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 215 3 2 2 1.9 O=c1cc(O)cc(CCc2ccccc2)[nH]1 10.1021/acs.jmedchem.3c01923
172468461 389242 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc[n+]([O-])c1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00951
CHEMBL5435126 389242 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc[n+]([O-])c1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00951
172468461 389242 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc[n+]([O-])c1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00951
CHEMBL5435126 389242 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc[n+]([O-])c1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00951
127044607 278381 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 238 8 2 4 3.2 CCCCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827526 278381 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 238 8 2 4 3.2 CCCCCCCCCc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
2969 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
2969 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayAgonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
10171 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
177643694 392178 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1ccccc1CCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5592070 392178 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 229 3 2 2 2.2 Cc1ccccc1CCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
9901435 314854 2 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 314 2 2 0 5.5 Clc1ccc2[nH]cc(Cc3c[nH]c4ccc(Cl)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4096406 314854 2 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 314 2 2 0 5.5 Clc1ccc2[nH]cc(Cc3c[nH]c4ccc(Cl)cc34)c2c1 10.1021/acs.jmedchem.6b01593
172449465 388376 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 285 3 0 2 3.7 [O-][n+]1cccc(COc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5415598 388376 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 285 3 0 2 3.7 [O-][n+]1cccc(COc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
10717 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
44349321 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL124977 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
10717 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
44349321 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL124977 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
11212 337 2 None -9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127045422 337 2 None -9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3828298 337 2 None -9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
177656403 391798 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574940 391798 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
178310829 467494 0 None None None Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 313 6 1 4 3.5 Oc1cc(CCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6177171 467494 0 None None None Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 313 6 1 4 3.5 Oc1cc(CCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
11208 2931 74 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
172449465 388376 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 285 3 0 2 3.7 [O-][n+]1cccc(COc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5415598 388376 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 285 3 0 2 3.7 [O-][n+]1cccc(COc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
177656732 391791 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574832 391791 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
10354234 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 by [35S]GTPgammaS binding assayAgonist activity at human GPR84 by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.6b01593
125356668 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 by [35S]GTPgammaS binding assayAgonist activity at human GPR84 by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.6b01593
5846 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 by [35S]GTPgammaS binding assayAgonist activity at human GPR84 by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.6b01593
CHEMBL3827832 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 by [35S]GTPgammaS binding assayAgonist activity at human GPR84 by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.6b01593
10354234 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
125356668 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
5846 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3827832 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
10354234 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11208 2931 74 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
11210 6531 3 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
146025748 6531 3 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL4538049 6531 3 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
8158 21242 67 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 158 7 1 1 2.8 CCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108436 21242 67 None None None Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 158 7 1 1 2.8 CCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
177656732 391791 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574832 391791 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 303 3 2 2 3.4 O=c1cc(O)cc(CCc2ccc3c(c2)Cc2ccccc2-3)[nH]1 10.1021/acs.jmedchem.3c01923
11213 2971 9 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
154578239 2971 9 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
CHEMBL4743442 2971 9 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
5850 207 53 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1039/C7MD00130D
94216 207 53 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1039/C7MD00130D
CHEMBL4288936 207 53 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1039/C7MD00130D
172440371 387446 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.3 O=C(CCc1cccc2ccccc12)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5396513 387446 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.3 O=C(CCc1cccc2ccccc12)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
137643701 314156 2 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
CHEMBL4088884 314156 2 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopyAgonist activity at human Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectroscopy
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.0c01378
172440371 387446 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.3 O=C(CCc1cccc2ccccc12)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5396513 387446 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 4 0 2 3.3 O=C(CCc1cccc2ccccc12)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
10171 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 4.3 pEC50 = 4.3 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
10171 3702 28 None None None Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1016/j.ejmech.2023.115762
71616860 3702 28 None None None Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1016/j.ejmech.2023.115762
CHEMBL3716365 3702 28 None None None Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1016/j.ejmech.2023.115762
DB15346 3702 28 None None None Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1016/j.ejmech.2023.115762
177656403 391798 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5574940 391798 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 233 5 2 2 2.8 CCCCCCCC#Cc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
176155025 392341 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
CHEMBL5594779 392341 0 None None None Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
12380289 314071 2 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4087824 314071 2 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
172454331 388435 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 5 0 2 4.3 COc1cc(CCCc2ccc(Cl)c3ccccc23)c[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5416844 388435 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 5 0 2 4.3 COc1cc(CCCc2ccc(Cl)c3ccccc23)c[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
172454331 388435 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 5 0 2 4.3 COc1cc(CCCc2ccc(Cl)c3ccccc23)c[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5416844 388435 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 327 5 0 2 4.3 COc1cc(CCCc2ccc(Cl)c3ccccc23)c[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
156499983 467481 0 None None None Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6176923 467481 0 None None None Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
127045635 278452 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 262 5 2 5 2.6 Oc1cc(O)nc(SCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828415 278452 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 262 5 2 5 2.6 Oc1cc(O)nc(SCCCc2ccccc2)n1 10.1021/acsmedchemlett.6b00025
156499996 467029 0 None None None Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 336 11 2 5 4.5 CCCCCCCCNc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6166866 467029 0 None None None Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 336 11 2 5 4.5 CCCCCCCCNc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
169561646 389741 0 None None None Human 5.2 pEC50 = 5.2 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 5.2 pEC50 = 5.2 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
172441513 387526 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 248 4 1 2 2.6 [O-][n+]1cccc(NCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5397948 387526 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 248 4 1 2 2.6 [O-][n+]1cccc(NCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
11208 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting methodAgonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
172441513 387526 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 248 4 1 2 2.6 [O-][n+]1cccc(NCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5397948 387526 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 248 4 1 2 2.6 [O-][n+]1cccc(NCCc2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.3c00951
127044299 278443 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 5 2.7 CCCCCCCCNc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828303 278443 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 5 2.7 CCCCCCCCNc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
177648470 392091 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5590375 392091 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
177652635 391744 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5574017 391744 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
172460033 388612 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 5 0 2 3.2 CCc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5420353 388612 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 5 0 2 3.2 CCc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
178323771 467311 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 405 20 1 3 8.4 CCCCCCCCCCCCOc1cc(O)cc(CCCCCCCCC)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6173567 467311 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 405 20 1 3 8.4 CCCCCCCCCCCCOc1cc(O)cc(CCCCCCCCC)n1 10.1021/acs.jmedchem.4c02335
178310161 467502 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 365 14 1 5 4.7 CCCCCCCCCc1cc(O)cc(OCCOCC2CCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6177379 467502 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 365 14 1 5 4.7 CCCCCCCCCc1cc(O)cc(OCCOCC2CCCO2)n1 10.1021/acs.jmedchem.4c02335
172460033 388612 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 5 0 2 3.2 CCc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
CHEMBL5420353 388612 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 277 5 0 2 3.2 CCc1cc(OCCc2ccc[n+]([O-])c2)ccc1Cl 10.1021/acs.jmedchem.3c00951
10171 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
169561646 389741 0 None None None Human 6.2 pEC50 = 6.2 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 6.2 pEC50 = 6.2 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.217 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
178306086 467176 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 13 1 4 5.5 CCCCCCCCCc1cc(O)cc(OCCOc2ccccc2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6170562 467176 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 13 1 4 5.5 CCCCCCCCCc1cc(O)cc(OCCOc2ccccc2)n1 10.1021/acs.jmedchem.4c02335
156499939 467006 0 None None None Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 4.3 CCCc1ccc(OCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6166272 467006 0 None None None Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 4.3 CCCc1ccc(OCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
172466600 389291 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(F)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5436093 389291 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(F)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
72711216 313652 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4082668 313652 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
11208 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None 2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
140898896 390717 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5556864 390717 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 243 4 2 2 3.1 CCCCc1ccc(-c2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
172466600 389291 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(F)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5436093 389291 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(F)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
11209 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
11209 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
127043349 278438 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 228 5 2 5 2.4 CC(C)CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828230 278438 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 228 5 2 5 2.4 CC(C)CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
137643701 314156 2 None -2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.03 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.03 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None -2 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.03 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.03 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
10354234 335 45 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
125356668 335 45 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
5846 335 45 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
CHEMBL3827832 335 45 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acsmedchemlett.6b00025
127045480 278436 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 3 2 5 1.8 CCC#CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828212 278436 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 3 2 5 1.8 CCC#CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
10171 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
172449541 387997 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc(Cl)cc1)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5408077 387997 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc(Cl)cc1)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
178323287 467393 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 265 10 1 2 4.1 CCCCCCCCCc1cc(OCC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6175198 467393 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 265 10 1 2 4.1 CCCCCCCCCc1cc(OCC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
172449541 387997 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc(Cl)cc1)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
CHEMBL5408077 387997 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 261 4 0 2 2.8 O=C(CCc1ccc(Cl)cc1)c1ccc[n+]([O-])c1 10.1021/acs.jmedchem.3c00951
177665986 391696 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 221 8 1 1 3.7 CCCCCCCCCc1cccc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5573140 391696 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 221 8 1 1 3.7 CCCCCCCCCc1cccc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11210 6531 3 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
146025748 6531 3 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
CHEMBL4538049 6531 3 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.3c00951
178323308 467291 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 321 11 1 3 4.2 CCCCCCCCCc1cc(OCC2CCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL6173132 467291 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 321 11 1 3 4.2 CCCCCCCCCc1cc(OCC2CCCO2)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
13892 8446 3 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499897 8446 3 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
CHEMBL6161601 8446 3 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499886 467445 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 369 9 1 4 4.9 CCCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176292 467445 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 369 9 1 4 4.9 CCCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
11208 2931 74 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 minsAgonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
8158 21242 67 None None None Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 158 7 1 1 2.8 CCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108436 21242 67 None None None Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 158 7 1 1 2.8 CCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
177655957 391721 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5573446 391721 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assayAgonist activity at GPR84 (unknown origin) expressed in doxycycline induced Flp-In-T-REx-293 cells transfected with GalphaI preincubated for 15 mins in presence of IBMX followed by forskolin stimulation for 45 mins by time-resolved fluorescence assay
ChEMBL 291 4 2 2 3.5 O=c1cc(O)cc(CCc2ccc(-c3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
177653966 391699 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5573172 391699 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 259 5 2 3 2.3 CCOc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
2969 2799 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
5532 2799 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL107498 2799 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
DB03600 2799 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
172459598 388562 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 4 0 2 4.1 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c[n+]1[O-] 10.1021/acs.jmedchem.3c00951
CHEMBL5419327 388562 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 4 0 2 4.1 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c[n+]1[O-] 10.1021/acs.jmedchem.3c00951
178317355 466388 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6144284 466388 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
172459598 388562 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 4 0 2 4.1 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c[n+]1[O-] 10.1021/acs.jmedchem.3c00951
CHEMBL5419327 388562 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 313 4 0 2 4.1 Cc1ccc(CCOc2ccc(Cl)c3ccccc23)c[n+]1[O-] 10.1021/acs.jmedchem.3c00951
5533 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
8180 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108030 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
172452408 387906 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 351 4 0 2 4.0 [O-][n+]1cccc(CCOc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5406066 387906 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 351 4 0 2 4.0 [O-][n+]1cccc(CCOc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
172452408 387906 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 351 4 0 2 4.0 [O-][n+]1cccc(CCOc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5406066 387906 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 351 4 0 2 4.0 [O-][n+]1cccc(CCOc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
11209 3191 70 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
3218 3191 70 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL221137 3191 70 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
177638153 390616 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.4 Cc1ccc(OCCCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5555365 390616 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 259 5 2 3 2.4 Cc1ccc(OCCCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
178307663 467102 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 343 7 1 5 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6168786 467102 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 343 7 1 5 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
172452623 388148 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 297 4 0 1 4.3 [O-][n+]1cccc(CCCc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5411044 388148 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 297 4 0 1 4.3 [O-][n+]1cccc(CCCc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
172452623 388148 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 297 4 0 1 4.3 [O-][n+]1cccc(CCCc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5411044 388148 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 297 4 0 1 4.3 [O-][n+]1cccc(CCCc2ccc(Cl)c3ccccc23)c1 10.1021/acs.jmedchem.3c00951
156500033 467452 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176351 467452 0 None None None Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
9882204 315330 21 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4101728 315330 21 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
169561646 389741 0 None None None Human 4.1 pEC50 = 4.1 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 4.1 pEC50 = 4.1 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 11.72 microM)
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
127044300 278417 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 7 2 4 2.8 CCCCCCCCc1cc(O)nc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3827933 278417 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 224 7 2 4 2.8 CCCCCCCCc1cc(O)nc(O)n1 10.1021/acsmedchemlett.6b00025
172452339 388428 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 375 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(I)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5416693 388428 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 375 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(I)c2)c1 10.1021/acs.jmedchem.3c00951
172452339 388428 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 375 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(I)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5416693 388428 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 375 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(I)c2)c1 10.1021/acs.jmedchem.3c00951
156499902 467432 0 None None None Human 6.1 pEC50 = 6.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 5.1 CCCCCc1ccc(-c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176041 467432 0 None None None Human 6.1 pEC50 = 6.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 355 8 1 4 5.1 CCCCCc1ccc(-c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
11208 2931 74 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.1 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
153309768 385373 0 None None None Human 4.1 pEC50 = 4.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None None None Human 4.1 pEC50 = 4.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
5533 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
8180 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108030 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
156499989 467226 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.7 CCCc1ccc(CCc2cc(O)cc(OCC3OCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6171578 467226 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.7 CCCc1ccc(CCc2cc(O)cc(OCC3OCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
156499923 467406 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 334 11 2 4 5.1 CCCCCCCCCc1cc(O)cc(NCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6175417 467406 0 None None None Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 334 11 2 4 5.1 CCCCCCCCCc1cc(O)cc(NCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
176155025 392341 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
CHEMBL5594779 392341 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting methodAgonist activity at GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by Topcount scintillation counting method
ChEMBL 251 9 1 3 4.1 CCCCCCCCCc1cc(O)cc(OC)n1 10.1021/acs.jmedchem.3c01923
3893 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 minsAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
4642 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 minsAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
5534 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 minsAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL108766 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 minsAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
DB03017 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 minsAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
127044151 278429 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 244 4 2 4 2.2 CCc1ccc(CCc2nc(O)cc(O)n2)cc1 10.1021/acsmedchemlett.6b00025
CHEMBL3828073 278429 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 244 4 2 4 2.2 CCc1ccc(CCc2nc(O)cc(O)n2)cc1 10.1021/acsmedchemlett.6b00025
3893 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
4642 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
5534 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
CHEMBL108766 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
DB03017 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assayAgonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.0c01378
127044950 278343 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 3 2 5 1.0 C#CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3826992 278343 0 None None None Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 196 3 2 5 1.0 C#CCCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
3893 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
4642 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5534 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108766 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03017 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
11209 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.3c00951
3218 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.3c00951
CHEMBL221137 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.3c00951
11209 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
172458367 388469 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.6 [O-][n+]1cccc(CCOc2ccc(Cl)c(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5417372 388469 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.6 [O-][n+]1cccc(CCOc2ccc(Cl)c(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
172460810 388560 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5419261 388560 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2)c1 10.1021/acs.jmedchem.3c00951
172460810 388560 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5419261 388560 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 283 4 0 2 3.2 [O-][n+]1cccc(CCOc2ccc(Cl)c(Cl)c2)c1 10.1021/acs.jmedchem.3c00951
172458367 388469 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.6 [O-][n+]1cccc(CCOc2ccc(Cl)c(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5417372 388469 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 317 4 0 2 3.6 [O-][n+]1cccc(CCOc2ccc(Cl)c(C(F)(F)F)c2)c1 10.1021/acs.jmedchem.3c00951
11211 8982 40 None -16 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
1912564 8982 40 None -16 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3827756 8982 40 None -16 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assayAgonist activity at GPR84 (unknown origin) expressed in HTLA cells assessed as beta-arrestin recruitment incubated for 1 day by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
11211 8982 40 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
1912564 8982 40 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3827756 8982 40 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
177652635 391744 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5574017 391744 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assayAgonist activity at GPR84 (unknown origin) expressed in HEK293T cells expressing beta-arrestin 2-nanoluciferase incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 271 5 2 2 3.1 CC(C)Cc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
10171 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
71616860 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL3716365 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
DB15346 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 300 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 microM)
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.3c00053
10171 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysisAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 100 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
156500127 467062 0 None None None Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 8 1 5 4.1 CCCc1ccc(CCc2cc(O)cc(OCC3OCCC(C)O3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6167776 467062 0 None None None Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayInverse agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 371 8 1 5 4.1 CCCc1ccc(CCc2cc(O)cc(OCC3OCCC(C)O3)n2)cc1 10.1021/acs.jmedchem.4c02335
127045481 278426 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 226 5 2 5 2.3 CC/C=C\CCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
CHEMBL3828033 278426 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 226 5 2 5 2.3 CC/C=C\CCSc1nc(O)cc(O)n1 10.1021/acsmedchemlett.6b00025
176155018 391783 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 251 9 1 2 3.7 CCCCCCCCCc1cc(OC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL5574706 391783 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assayAgonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment incubated for 30 mins by PRESTO-Tango assay
ChEMBL 251 9 1 2 3.7 CCCCCCCCCc1cc(OC)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
12530 20123 64 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107874 20123 64 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB02448 20123 64 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
172453677 388121 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 341 4 0 2 2.5 [O-][n+]1cccc(CCOc2ccc(I)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5410540 388121 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 341 4 0 2 2.5 [O-][n+]1cccc(CCOc2ccc(I)cc2)c1 10.1021/acs.jmedchem.3c00951
172453677 388121 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 341 4 0 2 2.5 [O-][n+]1cccc(CCOc2ccc(I)cc2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5410540 388121 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 341 4 0 2 2.5 [O-][n+]1cccc(CCOc2ccc(I)cc2)c1 10.1021/acs.jmedchem.3c00951
102219032 313261 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 274 2 2 0 4.9 Cc1cccc2[nH]cc(Cc3c[nH]c4cccc(C)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4077871 313261 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay
ChEMBL 274 2 2 0 4.9 Cc1cccc2[nH]cc(Cc3c[nH]c4cccc(C)c34)c12 10.1021/acs.jmedchem.6b01593
172463022 388865 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 289 5 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 10.1021/acs.jmedchem.3c00951
CHEMBL5426206 388865 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay
ChEMBL 289 5 0 2 3.5 [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 10.1021/acs.jmedchem.3c00951
90242131 271132 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3714891 271132 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
75203411 271139 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 392 4 0 7 2.7 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3714917 271139 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 392 4 0 7 2.7 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90239661 271140 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 474 6 0 10 3.0 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)on1 nan
CHEMBL3714918 271140 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 474 6 0 10 3.0 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)on1 nan
76684759 271152 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
CHEMBL3714958 271152 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
90253121 271175 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 473 5 1 8 2.8 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715016 271175 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 473 5 1 8 2.8 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684682 271194 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 477 7 0 9 2.6 CC1(COCc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
CHEMBL3715069 271194 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 477 7 0 9 2.6 CC1(COCc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
76684887 271235 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3[N+](=O)[O-])ccc1-2 nan
CHEMBL3715210 271235 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3[N+](=O)[O-])ccc1-2 nan
90242140 271238 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1ccccc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3715227 271238 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1ccccc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
90240329 271252 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3cccc(Cl)c3)ccc1-2 nan
CHEMBL3715290 271252 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3cccc(Cl)c3)ccc1-2 nan
90240601 271254 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 6 0 9 2.4 N#CCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715307 271254 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 6 0 9 2.4 N#CCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684890 271281 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 526 6 0 9 3.9 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
CHEMBL3715436 271281 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 526 6 0 9 3.9 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
90239433 271302 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1cccc(OCCOc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3715513 271302 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1cccc(OCCOc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
90242113 271340 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 465 4 0 9 3.0 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3715639 271340 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 465 4 0 9 3.0 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
90242191 271342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 517 6 0 11 3.3 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
CHEMBL3715645 271342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 517 6 0 11 3.3 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
76685019 271343 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 5 0 9 2.0 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715646 271343 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 5 0 9 2.0 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90241754 271353 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 5 1 8 3.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
CHEMBL3715684 271353 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 5 1 8 3.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
90242197 271357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 3 1 8 2.2 CC(C)(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715691 271357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 3 1 8 2.2 CC(C)(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242312 271389 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 473 5 1 8 3.0 CCC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)CC nan
CHEMBL3715779 271389 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 473 5 1 8 3.0 CCC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)CC nan
76684894 271427 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 525 8 1 8 3.4 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)NCc1ccccc1 nan
CHEMBL3715925 271427 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 525 8 1 8 3.4 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)NCc1ccccc1 nan
90241367 271430 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 6 0 9 3.5 CCOc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3715943 271430 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 6 0 9 3.5 CCOc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
127024685 271442 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 545 9 1 12 2.1 CCCn1nnnc1NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3715985 271442 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 545 9 1 12 2.1 CCCn1nnnc1NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
76685016 271443 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 530 8 0 10 4.0 CCOC(=O)c1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ccccc4O3)nc2=O)o1 nan
CHEMBL3715990 271443 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 530 8 0 10 4.0 CCOC(=O)c1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ccccc4O3)nc2=O)o1 nan
90241697 271479 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1ccccc1OCCOc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3716125 271479 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1ccccc1OCCOc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
76684889 271497 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 6 0 9 3.4 CC(C)(C)OC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3716166 271497 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 6 0 9 3.4 CC(C)(C)OC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242169 271501 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 443 4 0 9 2.5 Cn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3716178 271501 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 443 4 0 9 2.5 Cn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
76684664 271505 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 342 4 0 6 2.4 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCCO2)nc1=O nan
CHEMBL3716185 271505 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 342 4 0 6 2.4 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCCO2)nc1=O nan
76685018 271510 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 7 0 9 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3noc(-c4ccccc4)n3)ccc1-2 nan
CHEMBL3716202 271510 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 7 0 9 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3noc(-c4ccccc4)n3)ccc1-2 nan
90239903 271519 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 4 0 8 3.3 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccoc3)ccc1-2 nan
CHEMBL3716242 271519 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 4 0 8 3.3 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccoc3)ccc1-2 nan
76685012 271521 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 434 7 0 7 3.6 COc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3716251 271521 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 434 7 0 7 3.6 COc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
90240535 271545 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 7 0 8 3.4 COC(=O)c1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3716311 271545 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 7 0 8 3.4 COC(=O)c1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
76684492 271562 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 6 0 8 2.2 CN(C)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3716369 271562 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 6 0 8 2.2 CN(C)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242224 271570 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 511 7 1 8 3.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)Nc1ccccc1 nan
CHEMBL3716399 271570 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 511 7 1 8 3.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)Nc1ccccc1 nan
127024189 271580 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 559 10 1 12 2.5 CCCCn1nnnc1NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3716438 271580 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 559 10 1 12 2.5 CCCCn1nnnc1NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242703 271582 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 6 0 9 3.8 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1OC nan
CHEMBL3716443 271582 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 6 0 9 3.8 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1OC nan
76684665 271591 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3716482 271591 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
90241463 271632 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 6 0 9 3.8 COc1ccc(OC)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
CHEMBL3716622 271632 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 6 0 9 3.8 COc1ccc(OC)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
90253113 271662 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1ccccc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3716734 271662 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1ccccc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
76684577 271669 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCC3CCCO3)ccc1-2 nan
CHEMBL3716761 271669 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCC3CCCO3)ccc1-2 nan
90253082 271684 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 4 2 8 1.1 NC(=O)NCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716815 271684 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 4 2 8 1.1 NC(=O)NCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242227 271688 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 4 1 8 2.2 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716828 271688 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 4 1 8 2.2 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684578 271720 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3716925 271720 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
90241694 271721 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 503 7 0 11 3.2 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
CHEMBL3716930 271721 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 503 7 0 11 3.2 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
90240538 271749 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 6 0 9 3.5 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717010 271749 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 6 0 9 3.5 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242083 271767 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 501 7 0 11 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
CHEMBL3717081 271767 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 501 7 0 11 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
90240045 271794 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 440 4 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccncc3)ccc1-2 nan
CHEMBL3717169 271794 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 440 4 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccncc3)ccc1-2 nan
90242133 271814 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 6 1 10 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(NCc3ncco3)ccc1-2 nan
CHEMBL3717255 271814 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 6 1 10 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(NCc3ncco3)ccc1-2 nan
90241718 271818 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717267 271818 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242208 271829 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc(Cl)cc3)ccc1-2 nan
CHEMBL3717318 271829 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc(Cl)cc3)ccc1-2 nan
90253075 271831 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 506 8 0 10 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COCCN3CCOCC3)ccc1-2 nan
CHEMBL3717323 271831 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 506 8 0 10 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COCCN3CCOCC3)ccc1-2 nan
76684765 271833 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 7 0 8 2.9 CC(C)N(C)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3717326 271833 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 7 0 8 2.9 CC(C)N(C)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242015 271844 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc([N+](=O)[O-])cc3)ccc1-2 nan
CHEMBL3717358 271844 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc([N+](=O)[O-])cc3)ccc1-2 nan
90242171 271876 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 500 7 0 11 2.6 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnnn3C3CC3)ccc1-2 nan
CHEMBL3717472 271876 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 500 7 0 11 2.6 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnnn3C3CC3)ccc1-2 nan
76685013 271914 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 454 6 0 6 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc4ccccc4c3)ccc1-2 nan
CHEMBL3717594 271914 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 454 6 0 6 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc4ccccc4c3)ccc1-2 nan
76684489 271933 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccc(Cl)cc3)ccc1-2 nan
CHEMBL3717664 271933 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccc(Cl)cc3)ccc1-2 nan
76684573 271943 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 6 1 8 2.3 CC(C)(Oc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)C(N)=O nan
CHEMBL3717695 271943 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 6 1 8 2.3 CC(C)(Oc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)C(N)=O nan
76684667 271950 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 471 7 0 8 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4ccoc4)n3)ccc1-2 nan
CHEMBL3717729 271950 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 471 7 0 8 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4ccoc4)n3)ccc1-2 nan
90242431 271964 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 363 3 0 7 2.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1ccccc1-2 nan
CHEMBL3717782 271964 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 363 3 0 7 2.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1ccccc1-2 nan
76685010 271966 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3717786 271966 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
90242313 271974 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 477 6 0 9 3.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
CHEMBL3717805 271974 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 477 6 0 9 3.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
90240227 272010 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 4 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C3=CCOCC3)ccc1-2 nan
CHEMBL3717958 272010 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 445 4 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C3=CCOCC3)ccc1-2 nan
90241655 272036 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 475 6 0 11 2.4 Cc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
CHEMBL3718050 272036 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 475 6 0 11 2.4 Cc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
76684767 272043 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 0 8 2.6 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3718064 272043 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 0 8 2.6 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
76684888 272068 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 469 6 0 8 3.7 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3718158 272068 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 469 6 0 8 3.7 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
90253118 272073 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 525 5 0 10 3.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
CHEMBL3718169 272073 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 525 5 0 10 3.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
90241657 272085 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 444 4 0 8 2.0 CN(C)CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718203 272085 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 444 4 0 8 2.0 CN(C)CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684681 272096 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 6 0 9 2.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
CHEMBL3718246 272096 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 6 0 9 2.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
90242333 272100 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 7 0 9 2.4 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCOCC3)ccc1-2 nan
CHEMBL3718258 272100 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 7 0 9 2.4 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCOCC3)ccc1-2 nan
90240406 272111 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 504 5 0 9 3.8 COc1nccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1Cl nan
CHEMBL3718281 272111 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 504 5 0 9 3.8 COc1nccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1Cl nan
90242041 272120 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 11 2.6 CCc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
CHEMBL3718294 272120 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 11 2.6 CCc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)no1 nan
90242190 272124 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 493 4 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC(O)c3ccccc3)ccc1-2 nan
CHEMBL3718309 272124 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 493 4 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC(O)c3ccccc3)ccc1-2 nan
90242242 272147 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc([N+](=O)[O-])c3)ccc1-2 nan
CHEMBL3718388 272147 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc([N+](=O)[O-])c3)ccc1-2 nan
90242259 272170 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 4 1 8 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cn[nH]c3)ccc1-2 nan
CHEMBL3718482 272170 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 4 1 8 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cn[nH]c3)ccc1-2 nan
76684671 272179 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 447 7 1 7 3.0 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O)Nc1ccccc1 nan
CHEMBL3718511 272179 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 447 7 1 7 3.0 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O)Nc1ccccc1 nan
90242243 272181 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 5 0 9 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCOCC3)ccc1-2 nan
CHEMBL3718521 272181 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 5 0 9 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCOCC3)ccc1-2 nan
76684575 272186 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 448 9 0 7 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOCc3ccccc3)ccc1-2 nan
CHEMBL3718543 272186 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 448 9 0 7 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOCc3ccccc3)ccc1-2 nan
90242373 272199 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 497 5 1 9 2.5 CNC(=O)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3718580 272199 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 497 5 1 9 2.5 CNC(=O)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
90240336 272206 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 427 3 0 7 2.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3718614 272206 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 427 3 0 7 2.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
76684490 272211 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 505 6 0 9 1.9 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCOCC1 nan
CHEMBL3718620 272211 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 505 6 0 9 1.9 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCOCC1 nan
76684761 272224 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(Cl)c3)ccc1-2 nan
CHEMBL3718642 272224 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(Cl)c3)ccc1-2 nan
76684568 272233 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 6 0 6 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3)ccc1-2 nan
CHEMBL3718668 272233 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 6 0 6 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3)ccc1-2 nan
90240938 272237 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 506 6 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
CHEMBL3718687 272237 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 506 6 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
90242357 272240 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 4 1 8 2.4 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718693 272240 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 4 1 8 2.4 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684488 272261 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3Cl)ccc1-2 nan
CHEMBL3718767 272261 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 468 8 0 7 4.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3Cl)ccc1-2 nan
90239965 272276 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 4 0 8 3.6 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
CHEMBL3718808 272276 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 4 0 8 3.6 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
90242390 272280 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 5 1 8 2.6 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718814 272280 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 5 1 8 2.6 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76685017 272316 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3718963 272316 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
90242630 272328 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 471 5 0 10 2.5 COc1ncc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3719011 272328 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 471 5 0 10 2.5 COc1ncc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
90241703 272329 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 5 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCCC3)ccc1-2 nan
CHEMBL3719012 272329 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 5 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCCC3)ccc1-2 nan
76684663 272338 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 434 8 0 7 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3)ccc1-2 nan
CHEMBL3719036 272338 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 434 8 0 7 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3)ccc1-2 nan
90242134 272340 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 452 6 0 9 3.3 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)no1 nan
CHEMBL3719047 272340 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 452 6 0 9 3.3 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)no1 nan
76684768 272342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 1 10 1.8 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
CHEMBL3719052 272342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 1 10 1.8 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
90242408 272346 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1cncc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
CHEMBL3719065 272346 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1cncc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
76685015 272363 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1ccc(OCCOc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3719113 272363 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 464 9 0 8 3.5 COc1ccc(OCCOc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
90241653 272399 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 507 4 1 8 3.3 CC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)c1ccccc1 nan
CHEMBL3719248 272399 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 507 4 1 8 3.3 CC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)c1ccccc1 nan
76684491 272411 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 435 6 1 8 1.5 NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3719276 272411 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 435 6 1 8 1.5 NC(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
76684579 272424 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 461 6 1 11 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
CHEMBL3719334 272424 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 461 6 1 11 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
90241586 272425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 431 3 1 8 1.8 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3719339 272425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 431 3 1 8 1.8 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90240936 271216 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 440 4 0 8 2.7 N#CCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715145 271216 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 440 4 0 8 2.7 N#CCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90240635 271244 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 482 5 1 8 2.8 NC(=O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
CHEMBL3715263 271244 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 482 5 1 8 2.8 NC(=O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)c1 nan
90242118 271292 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 431 4 1 8 1.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCCO)ccc1-2 nan
CHEMBL3715466 271292 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 431 4 1 8 1.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCCO)ccc1-2 nan
90242136 271318 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 443 3 0 7 3.5 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715561 271318 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 443 3 0 7 3.5 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90241450 271437 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3715970 271437 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 470 5 0 9 3.2 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
90242112 271715 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 417 3 1 8 1.4 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCO)ccc1-2 nan
CHEMBL3716912 271715 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 417 3 1 8 1.4 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCO)ccc1-2 nan
76685021 271789 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 479 4 1 8 3.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc4[nH]ncc4c3)ccc1-2 nan
CHEMBL3717155 271789 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 479 4 1 8 3.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc4[nH]ncc4c3)ccc1-2 nan
90242324 271995 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 487 6 0 10 2.7 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)nn1C nan
CHEMBL3717888 271995 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 487 6 0 10 2.7 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)nn1C nan
90240696 272013 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 440 4 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 nan
CHEMBL3717964 272013 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 440 4 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 nan
90240228 272032 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 441 4 0 9 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cncnc3)ccc1-2 nan
CHEMBL3718025 272032 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 441 4 0 9 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cncnc3)ccc1-2 nan
90239905 272044 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
CHEMBL3718068 272044 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
90242578 272125 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 475 6 0 11 2.4 Cc1noc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)n1 nan
CHEMBL3718310 272125 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 475 6 0 11 2.4 Cc1noc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)n1 nan
90242205 272185 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 454 4 0 8 3.5 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3718542 272185 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 454 4 0 8 3.5 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
76684770 272302 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 424 4 0 5 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccc4ccccc4c3)ccc1-2 nan
CHEMBL3718872 272302 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 424 4 0 5 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccc4ccccc4c3)ccc1-2 nan
76684899 272377 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
CHEMBL3719180 272377 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
90242797 272393 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 471 3 1 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3(O)CCCC3)ccc1-2 nan
CHEMBL3719234 272393 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 471 3 1 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3(O)CCCC3)ccc1-2 nan
10171 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
71616860 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
CHEMBL3716365 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
DB15346 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
71617205 270441 2 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3719092 270441 2 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
71616756 271105 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 384 7 0 6 3.0 CCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3714783 271105 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 384 7 0 6 3.0 CCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
89645705 271106 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 6 0 7 2.8 CC(C)(C)COCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3714785 271106 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 6 0 7 2.8 CC(C)(C)COCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645448 271109 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 8 0 7 2.8 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCCCC3CC3)ccc1-2 nan
CHEMBL3714806 271109 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 8 0 7 2.8 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCCCC3CC3)ccc1-2 nan
71616163 271136 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3714904 271136 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616645 271191 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715064 271191 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616646 271199 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 384 6 0 7 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CC3)ccc1-2 nan
CHEMBL3715088 271199 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 384 6 0 7 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CC3)ccc1-2 nan
71616040 271230 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 420 3 0 6 3.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CCCCC3)ccc1-2 nan
CHEMBL3715192 271230 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 420 3 0 6 3.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CCCCC3)ccc1-2 nan
71615922 271283 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 5 0 7 2.6 CC(C)(C)OCc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715443 271283 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 5 0 7 2.6 CC(C)(C)OCc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616529 271347 0 None 36 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
CHEMBL3715656 271347 0 None 36 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
89645519 271394 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 398 7 0 7 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CC3)ccc1-2 nan
CHEMBL3715817 271394 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 398 7 0 7 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CC3)ccc1-2 nan
89645718 271420 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
CHEMBL3715907 271420 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
71617444 271426 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 3 0 6 2.7 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715923 271426 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 3 0 6 2.7 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616284 271453 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 410 4 1 7 1.6 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3716024 271453 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 410 4 1 7 1.6 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645729 271478 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 0 8 1.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3COC3)ccc1-2 nan
CHEMBL3716123 271478 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 0 8 1.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3COC3)ccc1-2 nan
71616864 271493 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 7 2.2 CC(C)C(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716159 271493 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 7 2.2 CC(C)C(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645780 271504 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 8 0 7 2.2 COCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716184 271504 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 8 0 7 2.2 COCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645570 271534 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 447 8 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCNc3ccccc3)ccc1-2 nan
CHEMBL3716280 271534 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 447 8 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCNc3ccccc3)ccc1-2 nan
89645206 271583 0 None 50 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 nan
CHEMBL3716446 271583 0 None 50 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 nan
89645671 271605 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCCC3)ccc1-2 nan
CHEMBL3716527 271605 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCCC3)ccc1-2 nan
89645393 271606 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 8 0 7 2.9 COC(CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O)C(C)C nan
CHEMBL3716528 271606 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 8 0 7 2.9 COC(CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O)C(C)C nan
71616863 271615 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 413 7 1 7 3.1 CCC(C)(C)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716561 271615 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 413 7 1 7 3.1 CCC(C)(C)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71615920 271657 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 9 2.3 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c(OC)n1 nan
CHEMBL3716722 271657 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 9 2.3 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c(OC)n1 nan
89645455 271660 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 474 5 0 8 3.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCCC4)nc3)ccc1-2 nan
CHEMBL3716728 271660 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 474 5 0 8 3.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCCC4)nc3)ccc1-2 nan
89645301 271674 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
CHEMBL3716784 271674 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
89645669 271705 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
CHEMBL3716889 271705 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
71616287 271732 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 457 6 1 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
CHEMBL3716958 271732 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 457 6 1 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
89645809 271769 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717086 271769 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616165 271803 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 nan
CHEMBL3717201 271803 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 nan
71616642 271855 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
CHEMBL3717416 271855 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
89645646 271917 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 0 7 3.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COC3CCCCC3)ccc1-2 nan
CHEMBL3717600 271917 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 0 7 3.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COC3CCCCC3)ccc1-2 nan
71616404 271926 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 410 5 1 7 1.8 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717641 271926 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 410 5 1 7 1.8 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616526 271952 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
CHEMBL3717743 271952 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
71616641 271957 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 445 4 1 8 1.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC(O)c3cccnc3)ccc1-2 nan
CHEMBL3717753 271957 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 445 4 1 8 1.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC(O)c3cccnc3)ccc1-2 nan
89645829 271958 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717755 271958 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645361 271968 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCOCC3)ccc1-2 nan
CHEMBL3717790 271968 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCOCC3)ccc1-2 nan
71616164 271969 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 5 0 6 2.8 CCCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717795 271969 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 5 0 6 2.8 CCCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645310 271976 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 1 7 2.6 CC(C)(C)C(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717809 271976 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 1 7 2.6 CC(C)(C)C(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616166 271986 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 1 7 2.0 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717853 271986 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 1 7 2.0 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71617677 271998 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 435 6 0 8 2.7 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717905 271998 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 435 6 0 8 2.7 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71617676 272012 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 8 2.9 COc1ccc(OC)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
CHEMBL3717963 272012 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 8 2.9 COc1ccc(OC)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
71616288 272027 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 409 6 1 8 2.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(NCc3ccco3)ccc1-2 nan
CHEMBL3718005 272027 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 409 6 1 8 2.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(NCc3ccco3)ccc1-2 nan
71617562 272048 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 476 5 0 9 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
CHEMBL3718080 272048 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 476 5 0 9 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
89645684 272082 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 467 6 0 9 3.1 CC(C)(C)c1cnc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)o1 nan
CHEMBL3718192 272082 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 467 6 0 9 3.1 CC(C)(C)c1cnc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)o1 nan
71615925 272095 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 487 7 0 9 3.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncc(-c4ccccc4)o3)ccc1-2 nan
CHEMBL3718244 272095 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 487 7 0 9 3.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncc(-c4ccccc4)o3)ccc1-2 nan
71616036 272128 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
CHEMBL3718331 272128 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
89645572 272135 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccccn3)ccc1-2 nan
CHEMBL3718350 272135 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccccn3)ccc1-2 nan
71616039 272174 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 406 3 0 6 2.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CCCC3)ccc1-2 nan
CHEMBL3718497 272174 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 406 3 0 6 2.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CCCC3)ccc1-2 nan
71615924 272182 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 460 5 0 8 2.9 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCC4)nc3)ccc1-2 nan
CHEMBL3718528 272182 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 460 5 0 8 2.9 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCC4)nc3)ccc1-2 nan
89645532 272209 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718618 272209 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645488 272248 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
CHEMBL3718720 272248 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
71617561 272324 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 435 6 0 8 2.7 CCOc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3718999 272324 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 435 6 0 8 2.7 CCOc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
89645626 272355 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 8 1 7 2.7 CCC(O)(CC)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3719080 272355 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 8 1 7 2.7 CCC(O)(CC)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645306 272359 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 0 7 2.2 COC(C)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3719100 272359 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 0 7 2.2 COC(C)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616035 272360 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 0 10 1.8 CCc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
CHEMBL3719101 272360 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 0 10 1.8 CCc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
89645377 272371 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
CHEMBL3719143 272371 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
71617560 272404 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 449 6 0 8 3.1 CC(C)Oc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3719258 272404 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 449 6 0 8 3.1 CC(C)Oc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71598639 272433 31 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3719364 272433 31 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
71616037 272435 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 454 7 0 10 2.3 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
CHEMBL3719374 272435 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 454 7 0 10 2.3 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
10171 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
71616860 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
CHEMBL3716365 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
DB15346 3702 28 None 125 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 nan
71616644 270438 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3717363 270438 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
71617205 270441 2 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3719092 270441 2 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
71616286 271127 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 458 4 1 7 2.5 CC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)c1ccccc1 nan
CHEMBL3714875 271127 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 458 4 1 7 2.5 CC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)c1ccccc1 nan
71616163 271136 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3714904 271136 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645754 271161 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
CHEMBL3714986 271161 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
89645653 271189 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 7 1 8 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCC(O)c3cccnc3)ccc1-2 nan
CHEMBL3715055 271189 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 7 1 8 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCC(O)c3cccnc3)ccc1-2 nan
71616645 271191 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715064 271191 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 3 0 6 2.3 CC(C)C#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71617203 271258 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 468 6 0 10 2.5 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
CHEMBL3715322 271258 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 468 6 0 10 2.5 CC(C)(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
71615922 271283 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 5 0 7 2.6 CC(C)(C)OCc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715443 271283 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 5 0 7 2.6 CC(C)(C)OCc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645316 271303 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 4 0 6 2.4 CCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715514 271303 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 380 4 0 6 2.4 CCCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616529 271347 0 None 36 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
CHEMBL3715656 271347 0 None 36 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 nan
89645442 271352 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 5 0 7 2.7 CC(C)(C)COc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715679 271352 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 5 0 7 2.7 CC(C)(C)COc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645718 271420 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
CHEMBL3715907 271420 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
89645365 271425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 nan
CHEMBL3715918 271425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 nan
71617444 271426 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 394 3 0 6 2.7 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715923 271426 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 394 3 0 6 2.7 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616284 271453 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 410 4 1 7 1.6 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3716024 271453 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 410 4 1 7 1.6 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645780 271504 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 8 0 7 2.2 COCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716184 271504 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 8 0 7 2.2 COCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645570 271534 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 447 8 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCNc3ccccc3)ccc1-2 nan
CHEMBL3716280 271534 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 447 8 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCNc3ccccc3)ccc1-2 nan
89645206 271583 0 None 50 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 nan
CHEMBL3716446 271583 0 None 50 2 Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 nan
89645671 271605 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 7 0 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCCC3)ccc1-2 nan
CHEMBL3716527 271605 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 7 0 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCCC3)ccc1-2 nan
71616863 271615 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 413 7 1 7 3.1 CCC(C)(C)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716561 271615 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 413 7 1 7 3.1 CCC(C)(C)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645455 271660 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 474 5 0 8 3.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCCC4)nc3)ccc1-2 nan
CHEMBL3716728 271660 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 474 5 0 8 3.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCCCC4)nc3)ccc1-2 nan
89645301 271674 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
CHEMBL3716784 271674 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
89645669 271705 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 428 6 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
CHEMBL3716889 271705 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 428 6 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCCCO3)ccc1-2 nan
89645809 271769 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717086 271769 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645506 271790 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
CHEMBL3717158 271790 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
71616165 271803 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 nan
CHEMBL3717201 271803 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 nan
71617672 271811 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 450 6 0 8 2.9 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1OC nan
CHEMBL3717251 271811 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 450 6 0 8 2.9 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1OC nan
89645546 271850 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 443 4 0 7 3.4 Cn1ccc2cc(-c3ccc4c(c3)CCn3c-4cc(OCC4COCCO4)nc3=O)ccc21 nan
CHEMBL3717390 271850 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 443 4 0 7 3.4 Cn1ccc2cc(-c3ccc4c(c3)CCn3c-4cc(OCC4COCCO4)nc3=O)ccc21 nan
71616642 271855 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
CHEMBL3717416 271855 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 nan
71616168 271869 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 396 4 1 7 1.4 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717453 271869 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 396 4 1 7 1.4 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616404 271926 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 410 5 1 7 1.8 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717641 271926 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 410 5 1 7 1.8 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645829 271958 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717755 271958 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645361 271968 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 428 6 0 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCOCC3)ccc1-2 nan
CHEMBL3717790 271968 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 428 6 0 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCC3CCOCC3)ccc1-2 nan
71617677 271998 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 435 6 0 8 2.7 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717905 271998 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 435 6 0 8 2.7 CCOc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645745 272003 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3717924 272003 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
71617562 272048 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 476 5 0 9 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
CHEMBL3718080 272048 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 476 5 0 9 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc(N4CCOCC4)nc3)ccc1-2 nan
89645443 272074 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 386 6 1 7 1.6 CC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718174 272074 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 386 6 1 7 1.6 CC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645513 272110 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 429 4 1 6 3.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc4[nH]ccc4c3)ccc1-2 nan
CHEMBL3718280 272110 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 429 4 1 6 3.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccc4[nH]ccc4c3)ccc1-2 nan
71616036 272128 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
CHEMBL3718331 272128 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 452 7 0 10 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 nan
89645497 272247 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 7 1 7 2.0 CC(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718719 272247 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 400 7 1 7 2.0 CC(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645488 272248 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
CHEMBL3718720 272248 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 382 6 0 6 2.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCC3CC3)ccc1-2 nan
89645319 272282 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 7 0 8 1.3 COCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718818 272282 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 426 7 0 8 1.3 COCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71617560 272404 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 6 0 8 3.1 CC(C)Oc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3719258 272404 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 6 0 8 3.1 CC(C)Oc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71598639 272433 31 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3719364 272433 31 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
71616037 272435 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 454 7 0 10 2.3 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
CHEMBL3719374 272435 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 454 7 0 10 2.3 CC(C)c1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
90242131 271132 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3714891 271132 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
76684759 271152 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
CHEMBL3714958 271152 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 462 6 0 8 3.2 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3COc4ccccc4O3)ccc1-2 nan
76684682 271194 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 477 7 0 9 2.6 CC1(COCc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
CHEMBL3715069 271194 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 477 7 0 9 2.6 CC1(COCc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
90240137 271301 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
CHEMBL3715503 271301 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
76685019 271343 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 418 5 0 9 2.0 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715646 271343 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 418 5 0 9 2.0 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242197 271357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 445 3 1 8 2.2 CC(C)(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715691 271357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 445 3 1 8 2.2 CC(C)(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90241450 271437 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 5 0 9 3.2 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3715970 271437 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 5 0 9 3.2 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
90242122 271602 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 431 4 0 8 2.1 COCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716520 271602 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 431 4 0 8 2.1 COCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242227 271688 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 445 4 1 8 2.2 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716828 271688 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 445 4 1 8 2.2 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684578 271720 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3716925 271720 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
90239525 271779 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 4 0 8 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717108 271779 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 4 0 8 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90253075 271831 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 506 8 0 10 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COCCN3CCOCC3)ccc1-2 nan
CHEMBL3717323 271831 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 506 8 0 10 1.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COCCN3CCOCC3)ccc1-2 nan
90242132 271936 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3717676 271936 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
90242324 271995 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 487 6 0 10 2.7 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)nn1C nan
CHEMBL3717888 271995 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 487 6 0 10 2.7 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)nn1C nan
90239905 272044 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
CHEMBL3718068 272044 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
76684681 272096 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 6 0 9 2.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
CHEMBL3718246 272096 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 6 0 9 2.0 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
90242242 272147 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc([N+](=O)[O-])c3)ccc1-2 nan
CHEMBL3718388 272147 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 449 7 0 8 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc([N+](=O)[O-])c3)ccc1-2 nan
90242259 272170 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 429 4 1 8 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cn[nH]c3)ccc1-2 nan
CHEMBL3718482 272170 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 429 4 1 8 2.5 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cn[nH]c3)ccc1-2 nan
90242205 272185 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 454 4 0 8 3.5 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
CHEMBL3718542 272185 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 454 4 0 8 3.5 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)cn1 nan
76684490 272211 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 505 6 0 9 1.9 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCOCC1 nan
CHEMBL3718620 272211 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 505 6 0 9 1.9 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCOCC1 nan
90240938 272237 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 506 6 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
CHEMBL3718687 272237 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 506 6 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCNCc3ccccc3)ccc1-2 nan
90242357 272240 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 459 4 1 8 2.4 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718693 272240 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 459 4 1 8 2.4 CC(C)C(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242390 272280 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 459 5 1 8 2.6 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718814 272280 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 459 5 1 8 2.6 CCCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76685017 272316 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3718963 272316 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
90241703 272329 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 5 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCCC3)ccc1-2 nan
CHEMBL3719012 272329 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 5 0 8 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCCC3)ccc1-2 nan
76684663 272338 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 434 8 0 7 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3)ccc1-2 nan
CHEMBL3719036 272338 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 434 8 0 7 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCOc3ccccc3)ccc1-2 nan
76684768 272342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 1 10 1.8 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
CHEMBL3719052 272342 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 460 6 1 10 1.8 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
76684892 272357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 489 6 0 8 2.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCCC1 nan
CHEMBL3719089 272357 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 489 6 0 8 2.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCCC1 nan
76684899 272377 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
CHEMBL3719180 272377 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 470 6 0 9 3.1 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
90242797 272393 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 3 1 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3(O)CCCC3)ccc1-2 nan
CHEMBL3719234 272393 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 3 1 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC3(O)CCCC3)ccc1-2 nan
90241586 272425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 431 3 1 8 1.8 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3719339 272425 0 None None None Human 11.0 pIC50 = 11 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 431 3 1 8 1.8 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242190 272124 0 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 493 4 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC(O)c3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3718309 272124 0 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 493 4 1 8 3.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CC(O)c3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c00272
71616529 271347 0 None 36 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
137636801 311823 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 464 3 0 8 2.9 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncn3)ccc1-2 10.1021/acs.jmedchem.6b00935
CHEMBL4060589 311823 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 464 3 0 8 2.9 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3ccncn3)ccc1-2 10.1021/acs.jmedchem.6b00935
137634047 312561 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 486 6 0 9 3.3 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)nn1C 10.1021/acs.jmedchem.6b00935
CHEMBL4069275 312561 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 486 6 0 9 3.3 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)nn1C 10.1021/acs.jmedchem.6b00935
137652440 313430 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 0 8 3.1 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cncnc3)ccc1-2 10.1021/acs.jmedchem.6b00935
CHEMBL4080004 313430 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 0 8 3.1 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cncnc3)ccc1-2 10.1021/acs.jmedchem.6b00935
137647203 313641 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 481 5 1 7 3.5 NC(=O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)c1 10.1021/acs.jmedchem.6b00935
CHEMBL4082477 313641 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 481 5 1 7 3.5 NC(=O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)c1 10.1021/acs.jmedchem.6b00935
137648721 313903 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 439 4 0 7 3.7 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 10.1021/acs.jmedchem.6b00935
CHEMBL4085616 313903 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 439 4 0 7 3.7 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 10.1021/acs.jmedchem.6b00935
137643534 314302 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 430 4 1 7 2.4 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCCO)ccc1-2 10.1021/acs.jmedchem.6b00935
CHEMBL4090321 314302 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 430 4 1 7 2.4 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCCO)ccc1-2 10.1021/acs.jmedchem.6b00935
137661584 314997 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 474 6 0 10 3.0 Cc1noc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)n1 10.1021/acs.jmedchem.6b00935
CHEMBL4098028 314997 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 474 6 0 10 3.0 Cc1noc(COc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)cc2=O)n1 10.1021/acs.jmedchem.6b00935
137657193 315470 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 478 4 1 7 4.2 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc4[nH]ncc4c3)ccc1-2 10.1021/acs.jmedchem.6b00935
CHEMBL4103552 315470 0 None None None Human 8.0 pIC50 = 8 Functional
Antagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assayAntagonist activity at GPR84 (unknown origin) expressed in cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 478 4 1 7 4.2 O=c1cc(OCC2COc3ncccc3O2)cc2n1CCc1cc(-c3ccc4[nH]ncc4c3)ccc1-2 10.1021/acs.jmedchem.6b00935
168277163 373719 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 433 6 2 4 4.9 CC(=O)NCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5181240 373719 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 433 6 2 4 4.9 CC(=O)NCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
76684896 271108 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 8 3.6 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCCCC3)ccc1-2 nan
CHEMBL3714804 271108 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 8 3.6 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCCCC3)ccc1-2 nan
90242245 271111 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 8 0 8 2.9 CCN(CC)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3714809 271111 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 491 8 0 8 2.9 CCN(CC)C(=O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242297 271117 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 444 3 1 8 2.2 CC(C)(N)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3714820 271117 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 444 3 1 8 2.2 CC(C)(N)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242183 271119 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 388 3 0 8 2.0 N#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3714825 271119 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 388 3 0 8 2.0 N#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684668 271133 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 483 7 0 9 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4cncnc4)n3)ccc1-2 nan
CHEMBL3714897 271133 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 483 7 0 9 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4cncnc4)n3)ccc1-2 nan
76685020 271143 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 490 7 0 9 2.9 CN1CCCC1CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3714922 271143 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 490 7 0 9 2.9 CN1CCCC1CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684763 271151 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 422 6 0 6 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc(F)cc3)ccc1-2 nan
CHEMBL3714952 271151 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 422 6 0 6 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccc(F)cc3)ccc1-2 nan
76684764 271198 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 7 0 8 3.4 COC(=O)c1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3715086 271198 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 462 7 0 8 3.4 COC(=O)c1ccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
76684669 271211 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 436 7 0 10 1.9 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3nnnn3C3CC3)ccc1-2 nan
CHEMBL3715120 271211 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 436 7 0 10 1.9 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3nnnn3C3CC3)ccc1-2 nan
90242048 271242 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 446 5 0 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCC3)ccc1-2 nan
CHEMBL3715250 271242 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 446 5 0 8 2.7 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(CN3CCCC3)ccc1-2 nan
76684672 271268 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3715368 271268 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
90242407 271312 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 3 1 8 3.1 NC1(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)CCCCC1 nan
CHEMBL3715550 271312 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 484 3 1 8 3.1 NC1(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)CCCCC1 nan
90242079 271339 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 534 4 0 10 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCN3CCS(=O)(=O)CC3)ccc1-2 nan
CHEMBL3715633 271339 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 534 4 0 10 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#CCN3CCS(=O)(=O)CC3)ccc1-2 nan
76684660 271386 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 7 0 6 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCc3ccccc3)ccc1-2 nan
CHEMBL3715772 271386 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 7 0 6 3.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCCc3ccccc3)ccc1-2 nan
90242088 271418 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 7 1 8 2.8 CCCCNCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3715903 271418 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 7 1 8 2.8 CCCCNCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242279 271466 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3716060 271466 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
76684675 271503 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 1 6 2.8 NC(=O)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3716183 271503 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 1 6 2.8 NC(=O)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
76684760 271528 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3716270 271528 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 429 6 0 7 3.5 N#Cc1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
76684895 271551 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 475 7 0 8 3.2 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCCC3)ccc1-2 nan
CHEMBL3716334 271551 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 475 7 0 8 3.2 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCN3CCCC3)ccc1-2 nan
76684762 271584 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3Cl)ccc1-2 nan
CHEMBL3716448 271584 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 6 0 6 4.3 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccc3Cl)ccc1-2 nan
90240503 271673 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 503 8 0 8 3.9 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCCN3CCCCC3)ccc1-2 nan
CHEMBL3716781 271673 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 503 8 0 8 3.9 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCCCN3CCCCC3)ccc1-2 nan
90242110 271678 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 8 0 10 2.0 CCCn1nnnc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3716807 271678 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 438 8 0 10 2.0 CCCn1nnnc1COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
90253097 271702 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 7 3.3 C=CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3716875 271702 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 6 0 7 3.3 C=CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
76684572 271810 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 370 7 0 6 3.2 CCCCOc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3717237 271810 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 370 7 0 6 3.2 CCCCOc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
76684891 271824 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 436 6 1 8 2.1 O=C(O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3717307 271824 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 436 6 1 8 2.1 O=C(O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242695 271839 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 4 1 9 1.0 O=C1CN(CC#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)C(=O)N1 nan
CHEMBL3717345 271839 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 499 4 1 9 1.0 O=C1CN(CC#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)C(=O)N1 nan
90242132 271936 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3717676 271936 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 460 6 0 10 2.6 O=c1nc(OC[C@@H]2COc3ncccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
90253148 272019 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 490 5 1 9 2.0 O=C(NC1CCOCC1)c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717979 272019 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 490 5 1 9 2.0 O=C(NC1CCOCC1)c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242347 272025 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 486 5 1 9 1.8 CCNC1(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
CHEMBL3717999 272025 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 486 5 1 9 1.8 CCNC1(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COc4ncccc4O3)nc2=O)COC1 nan
76684769 272026 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 6 0 9 3.3 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3718000 272026 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 459 6 0 9 3.3 O=c1nc(OCC2COc3ccccc3O2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
90242067 272035 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 6 0 8 2.8 CCN(CC)CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718037 272035 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 472 6 0 8 2.8 CCN(CC)CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242339 272055 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 7 0 10 1.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCCN3CCOCC3)ccc1-2 nan
CHEMBL3718109 272055 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 492 7 0 10 1.8 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCCN3CCOCC3)ccc1-2 nan
90241517 272080 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 8 3.5 CN1CCCC1CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3718190 272080 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 7 0 8 3.5 CN1CCCC1CCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
76684569 272099 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccnc3)ccc1-2 nan
CHEMBL3718257 272099 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccnc3)ccc1-2 nan
76684674 272123 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 0 6 3.8 CN(C)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
CHEMBL3718308 272123 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 0 6 3.8 CN(C)c1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cc1 nan
76684571 272151 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 368 6 0 6 2.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3CC3)ccc1-2 nan
CHEMBL3718406 272151 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 368 6 0 6 2.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3CC3)ccc1-2 nan
76684666 272164 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 485 7 0 9 3.4 Cn1cc(-c2cccc(COc3ccc4c(c3)CCn3c-4cc(OCC4CCCO4)nc3=O)n2)cn1 nan
CHEMBL3718451 272164 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 485 7 0 9 3.4 Cn1cc(-c2cccc(COc3ccc4c(c3)CCn3c-4cc(OCC4CCCO4)nc3=O)n2)cn1 nan
90241668 272198 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 518 8 0 9 2.7 CN1CCN(CCCOc2ccc3c(c2)CCn2c-3cc(OCC3COc4ccccc4O3)nc2=O)CC1 nan
CHEMBL3718572 272198 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 518 8 0 9 2.7 CN1CCN(CCCOc2ccc3c(c2)CCn2c-3cc(OCC3COc4ccccc4O3)nc2=O)CC1 nan
76684581 272207 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 399 4 0 6 3.6 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3718615 272207 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 399 4 0 6 3.6 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
90242241 272208 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3718616 272208 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 404 5 0 6 3.7 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
90242125 272226 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 1 9 2.0 N#CCNc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718644 272226 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 417 5 1 9 2.0 N#CCNc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76684582 272229 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 374 4 0 5 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccccc3)ccc1-2 nan
CHEMBL3718652 272229 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 374 4 0 5 3.7 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccccc3)ccc1-2 nan
76684662 272265 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
CHEMBL3718778 272265 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 nan
90242071 272326 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 520 6 0 8 3.6 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)Cc1ccccc1 nan
CHEMBL3719006 272326 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 520 6 0 8 3.6 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O)Cc1ccccc1 nan
76684892 272357 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 6 0 8 2.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCCC1 nan
CHEMBL3719089 272357 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 489 6 0 8 2.7 O=C(COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)N1CCCC1 nan
76684661 272434 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
CHEMBL3719373 272434 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 405 6 0 7 3.0 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ccncc3)ccc1-2 nan
90240137 271301 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
CHEMBL3715503 271301 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 3 0 8 2.9 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
76684775 271382 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 405 5 0 7 3.1 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cn1 nan
CHEMBL3715761 271382 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 405 5 0 7 3.1 COc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)cn1 nan
90240249 271441 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 393 4 0 7 3.3 Cc1noc(C)c1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3715983 271441 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 393 4 0 7 3.3 Cc1noc(C)c1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
90242122 271602 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 431 4 0 8 2.1 COCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716520 271602 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 431 4 0 8 2.1 COCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90239525 271779 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 4 0 8 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717108 271779 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 464 4 0 8 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90239807 271913 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 482 5 0 8 3.8 CN(C)c1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3717592 271913 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 482 5 0 8 3.8 CN(C)c1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90242403 272196 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 362 3 0 5 2.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3718569 272196 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 362 3 0 5 2.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
76684901 272246 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 469 5 0 8 3.8 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3718718 272246 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 469 5 0 8 3.8 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
76685011 272410 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3719274 272410 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 418 6 0 6 3.9 Cc1cccc(COc2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
71616971 272243 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3718710 272243 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
76684668 271133 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 483 7 0 9 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4cncnc4)n3)ccc1-2 nan
CHEMBL3714897 271133 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 483 7 0 9 3.5 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc(-c4cncnc4)n3)ccc1-2 nan
76684579 272424 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 461 6 1 11 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
CHEMBL3719334 272424 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human human buffy coat neutrophils assessed as inhibition of cell migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 461 6 1 11 1.2 O=c1nc(OCC2COc3ncccc3O2)cc2n1CCc1cc(OCc3nnn[nH]3)ccc1-2 nan
156500013 467404 0 None -35 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175409 467404 0 None -35 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
168283101 374092 0 None None None Human 5.0 pIC50 = 5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 338 5 0 4 4.4 c1ccc(-c2nnc(CCc3cccnc3)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5186775 374092 0 None None None Human 5.0 pIC50 = 5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 338 5 0 4 4.4 c1ccc(-c2nnc(CCc3cccnc3)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
71616644 270438 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
CHEMBL3717363 270438 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 nan
71616402 271112 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 7 0 8 3.2 CC(C)CCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3714813 271112 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 7 0 8 3.2 CC(C)CCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71617446 271120 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
CHEMBL3714827 271120 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccncc3)ccc1-2 nan
89645754 271161 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
CHEMBL3714986 271161 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 1 7 2.5 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(CCC3(O)CCCC3)ccc1-2 nan
127024072 271172 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 471 4 1 7 2.0 CNC(=O)c1ccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
CHEMBL3715009 271172 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 471 4 1 7 2.0 CNC(=O)c1ccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
89645653 271189 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 449 7 1 8 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCC(O)c3cccnc3)ccc1-2 nan
CHEMBL3715055 271189 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 449 7 1 8 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCC(O)c3cccnc3)ccc1-2 nan
89645308 271196 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 6 0 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(C#CCOCCF)ccc1-2 nan
CHEMBL3715080 271196 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 6 0 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(C#CCOCCF)ccc1-2 nan
71617094 271203 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 418 3 0 8 1.4 Cn1cncc1C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715095 271203 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 418 3 0 8 1.4 Cn1cncc1C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645726 271246 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 1 7 2.0 CCC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715265 271246 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 1 7 2.0 CCC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616968 271275 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715404 271275 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645698 271287 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 369 5 0 8 1.2 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715459 271287 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 369 5 0 8 1.2 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645638 271310 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 6 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NCC3CCCCC3)ccc1-2 nan
CHEMBL3715540 271310 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 6 1 7 3.3 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NCC3CCCCC3)ccc1-2 nan
71616403 271327 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 4 0 7 2.8 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)o1 nan
CHEMBL3715594 271327 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 394 4 0 7 2.8 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)o1 nan
89645442 271352 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 5 0 7 2.7 CC(C)(C)COc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715679 271352 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 5 0 7 2.7 CC(C)(C)COc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645405 271356 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 1 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCCO)ccc1-2 nan
CHEMBL3715690 271356 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 1 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(CCCCO)ccc1-2 nan
71616865 271410 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 441 10 1 7 3.9 CCCCC(CC)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3715870 271410 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 441 10 1 7 3.9 CCCCC(CC)CNc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71617557 271412 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 314 3 0 6 1.3 O=c1nc(OCC2COCCO2)cc2n1CCc1ccccc1-2 nan
CHEMBL3715879 271412 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 314 3 0 6 1.3 O=c1nc(OCC2COCCO2)cc2n1CCc1ccccc1-2 nan
89645365 271425 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 nan
CHEMBL3715918 271425 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 nan
71616528 271462 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 338 3 0 6 1.2 C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3716050 271462 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 338 3 0 6 1.2 C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
127024075 271477 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 444 4 0 7 2.7 COc1cccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
CHEMBL3716121 271477 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 444 4 0 7 2.7 COc1cccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
89645197 271491 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 7 2.4 CC(C)(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716157 271491 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 7 2.4 CC(C)(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71617443 271508 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1cc(F)cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
CHEMBL3716195 271508 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1cc(F)cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
89645383 271577 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 8 0 8 1.7 CCOCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716433 271577 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 440 8 0 8 1.7 CCOCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645355 271631 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 7 0 7 3.5 CC(C)(C)CCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716619 271631 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 7 0 7 3.5 CC(C)(C)CCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616643 271697 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 0 7 2.3 COC(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)C(C)C nan
CHEMBL3716857 271697 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 0 7 2.3 COC(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)C(C)C nan
71617322 271704 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1ccc(F)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
CHEMBL3716882 271704 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1ccc(F)c(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
71616861 271751 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 0 8 1.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
CHEMBL3717016 271751 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 0 8 1.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COC3COC3)ccc1-2 nan
89645265 271786 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 411 5 1 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NC3CCCCC3)ccc1-2 nan
CHEMBL3717133 271786 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 411 5 1 7 3.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NC3CCCCC3)ccc1-2 nan
89645506 271790 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
CHEMBL3717158 271790 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3cccnc3)ccc1-2 nan
71617672 271811 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 8 2.9 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1OC nan
CHEMBL3717251 271811 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 8 2.9 COc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1OC nan
86717362 271821 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3717285 271821 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 9 0 8 2.1 CCCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
89645412 271854 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 3 1 7 1.0 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717415 271854 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 3 1 7 1.0 CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616168 271869 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 396 4 1 7 1.4 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3717453 271869 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 396 4 1 7 1.4 CCC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616757 271875 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 458 6 1 8 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNCc3cccnc3)ccc1-2 nan
CHEMBL3717471 271875 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 458 6 1 8 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNCc3cccnc3)ccc1-2 nan
71616407 271877 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 422 6 0 8 2.5 CCCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3717473 271877 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 422 6 0 8 2.5 CCCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71616752 271899 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 402 8 0 8 1.7 CCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717561 271899 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 402 8 0 8 1.7 CCOCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616524 271970 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3717796 271970 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645745 272003 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3717924 272003 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 7 0 7 1.8 COCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
89645156 272014 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
CHEMBL3717967 272014 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
71616038 272022 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 0 10 1.5 Cc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
CHEMBL3717983 272022 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 6 0 10 1.5 Cc1nc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)no1 nan
71616973 272030 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 411 6 0 9 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3718012 272030 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 411 6 0 9 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
71616285 272034 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 1 7 2.2 CCC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)CC nan
CHEMBL3718036 272034 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 424 5 1 7 2.2 CCC(O)(C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)CC nan
71617448 272058 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 5 0 8 2.3 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3718113 272058 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 5 0 8 2.3 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645443 272074 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 6 1 7 1.6 CC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718174 272074 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 386 6 1 7 1.6 CC(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71617558 272114 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 396 4 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C3=CCOCC3)ccc1-2 nan
CHEMBL3718288 272114 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 396 4 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C3=CCOCC3)ccc1-2 nan
71616753 272115 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3718289 272115 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
71617445 272117 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 6 0 9 2.1 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)on1 nan
CHEMBL3718290 272117 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 6 0 9 2.1 Cc1cc(COc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)on1 nan
89645313 272129 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 418 4 0 8 1.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCn3ccnc3)ccc1-2 nan
CHEMBL3718332 272129 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 418 4 0 8 1.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCn3ccnc3)ccc1-2 nan
89645749 272149 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 1 7 2.0 CC(C)(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718393 272149 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 6 1 7 2.0 CC(C)(O)CCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616754 272153 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718413 272153 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 370 6 0 7 1.8 C=CCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
86688463 272162 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 344 4 0 7 1.3 COc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3718436 272162 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 344 4 0 7 1.3 COc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71616525 272235 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3718680 272235 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
71616971 272243 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3718710 272243 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645497 272247 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 1 7 2.0 CC(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718719 272247 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 400 7 1 7 2.0 CC(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616974 272273 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 388 7 0 8 1.3 COCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718802 272273 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 388 7 0 8 1.3 COCCOc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645319 272282 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 8 1.3 COCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3718818 272282 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 8 1.3 COCCOCC#Cc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
71616755 272284 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCOCC3)ccc1-2 nan
CHEMBL3718828 272284 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 6 0 8 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(COC3CCOCC3)ccc1-2 nan
71617675 272369 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 4 0 8 2.2 N#Cc1ccncc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3719137 272369 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 4 0 8 2.2 N#Cc1ccncc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
71617673 272429 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 455 5 0 8 3.0 COc1nccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1Cl nan
CHEMBL3719358 272429 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 455 5 0 8 3.0 COc1nccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1Cl nan
71616756 271105 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 384 7 0 6 3.0 CCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3714783 271105 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 384 7 0 6 3.0 CCCCCc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
127024072 271172 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 4 1 7 2.0 CNC(=O)c1ccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
CHEMBL3715009 271172 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 471 4 1 7 2.0 CNC(=O)c1ccc(C#Cc2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cc1 nan
71617094 271203 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 418 3 0 8 1.4 Cn1cncc1C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715095 271203 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 418 3 0 8 1.4 Cn1cncc1C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645698 271287 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 369 5 0 8 1.2 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715459 271287 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 369 5 0 8 1.2 N#CCOc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645270 271366 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 420 5 0 7 2.9 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3715719 271366 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 420 5 0 7 2.9 COc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645197 271491 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 414 7 1 7 2.4 CC(C)(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
CHEMBL3716157 271491 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 414 7 1 7 2.4 CC(C)(O)CCCc1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O nan
89645507 271930 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 405 4 0 7 2.6 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3717653 271930 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 405 4 0 7 2.6 Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71616973 272030 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 411 6 0 9 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3718012 272030 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 411 6 0 9 1.8 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
71617448 272058 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 421 5 0 8 2.3 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
CHEMBL3718113 272058 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 421 5 0 8 2.3 COc1ncccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O nan
89645572 272135 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccccn3)ccc1-2 nan
CHEMBL3718350 272135 0 None None None Human 7.0 pIC50 = 7 Functional
Antagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assayAntagonist activity against GPR84 in human buffy coat neutrophils assessed as reduction in neutrophils migration towards embelin pre-incubated for 30 mins and measured after 1 hr by ATPlite luminescence ATP detection assay
ChEMBL 415 3 0 7 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ccccn3)ccc1-2 nan
12918236 385591 1 None None None Human 5.0 pIC50 = 5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 350 4 1 3 5.6 O=P(O)(Oc1ccc2ccccc2c1)Oc1ccc2ccccc2c1 10.1021/acs.jmedchem.1c01813
CHEMBL5222969 385591 1 None None None Human 5.0 pIC50 = 5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 350 4 1 3 5.6 O=P(O)(Oc1ccc2ccccc2c1)Oc1ccc2ccccc2c1 10.1021/acs.jmedchem.1c01813
71616644 270438 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3717363 270438 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
156499925 467036 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.3 CCCc1ccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6167043 467036 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.3 CCCc1ccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168277748 373368 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5175634 373368 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
168287456 374568 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 286 3 1 3 3.6 c1ccc(-c2cnnc(Cc3c[nH]c4ccccc34)n2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5193872 374568 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 286 3 1 3 3.6 c1ccc(-c2cnnc(Cc3c[nH]c4ccccc34)n2)cc1 10.1021/acs.jmedchem.2c00804
178323398 467483 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 361 7 1 5 3.7 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1F 10.1021/acs.jmedchem.4c02335
CHEMBL6176993 467483 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 361 7 1 5 3.7 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1F 10.1021/acs.jmedchem.4c02335
153309768 385373 0 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
71616167 353665 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 354 4 0 6 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL4744625 353665 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 354 4 0 6 2.1 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
10171 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
71616860 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
CHEMBL3716365 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
DB15346 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
156499911 467398 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
CHEMBL6175294 467398 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
168283580 374299 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 327 4 1 4 3.8 Cc1cc(Cc2nnc(-c3ccccc3)c(-c3ccccc3)n2)n[nH]1 10.1021/acs.jmedchem.2c00804
CHEMBL5189932 374299 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 327 4 1 4 3.8 Cc1cc(Cc2nnc(-c3ccccc3)c(-c3ccccc3)n2)n[nH]1 10.1021/acs.jmedchem.2c00804
169561616 389805 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 448 11 1 5 7.2 CCCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499809 389805 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 448 11 1 5 7.2 CCCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
162642975 355500 0 None 67 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassayAntagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassay
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4776061 355500 0 None 67 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassayAntagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassay
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
147422825 385576 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 478 4 1 3 7.3 O=P(O)(OC1=Cc2ccccc2Cc2ccccc21)OC1=Cc2ccccc2Cc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222874 385576 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 478 4 1 3 7.3 O=P(O)(OC1=Cc2ccccc2Cc2ccccc21)OC1=Cc2ccccc2Cc2ccccc21 10.1021/acs.jmedchem.1c01813
163321284 373699 14 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 422 6 1 5 5.3 COc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5180892 373699 14 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 422 6 1 5 5.3 COc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
169561648 389697 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 5 1 5 7.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1C(C)(C)CCCC1(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5498943 389697 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 5 1 5 7.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1C(C)(C)CCCC1(C)C 10.1021/acs.jmedchem.3c00053
23110717 390560 7 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 528 2 1 3 9.5 Cc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5549984 390560 7 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 528 2 1 3 9.5 Cc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
10171 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None 125 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
168274895 373311 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 488 5 1 5 4.7 CN1CCN(C(=O)c2ccc(-c3nnc(Cc4c[nH]c5ccccc45)nc3-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.2c00804
CHEMBL5174701 373311 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 488 5 1 5 4.7 CN1CCN(C(=O)c2ccc(-c3nnc(Cc4c[nH]c5ccccc45)nc3-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.2c00804
153309805 385474 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2ccc(Cl)cc2Sc2ccccc21)OC1=Cc2ccc(Cl)cc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222262 385474 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2ccc(Cl)cc2Sc2ccccc21)OC1=Cc2ccc(Cl)cc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
178323465 467361 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 8 1 6 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)c(OC)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6174652 467361 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 8 1 6 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)c(OC)c1 10.1021/acs.jmedchem.4c02335
168292024 375055 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5201724 375055 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
162672502 366465 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 352 4 0 5 3.2 COc1ccc2c(c1)CCn1c-2cc(OCc2ccccc2F)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL4794623 366465 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 352 4 0 5 3.2 COc1ccc2c(c1)CCn1c-2cc(OCc2ccccc2F)nc1=O 10.1021/acs.jmedchem.0c00272
168272510 373329 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 433 6 2 4 4.9 CC(=O)NCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5174990 373329 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 433 6 2 4 4.9 CC(=O)NCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
178323088 467424 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 9 1 6 3.8 CCOc1ccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6175896 467424 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 9 1 6 3.8 CCOc1ccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
149469204 375057 0 None 4 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 3-OH-C12 induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 3-OH-C12 induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5201755 375057 0 None 4 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 3-OH-C12 induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 3-OH-C12 induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
169561532 389710 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 526 5 1 5 7.9 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC(F)(F)F)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499028 389710 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 526 5 1 5 7.9 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC(F)(F)F)cccc21 10.1021/acs.jmedchem.3c00053
168277450 373599 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 6 1 5 5.4 COc1ccc(-c2nnc(Cc3c[nH]c4ccc(F)cc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5179431 373599 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 6 1 5 5.4 COc1ccc(-c2nnc(Cc3c[nH]c4ccc(F)cc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
168286683 374668 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4ncccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5195409 374668 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4ncccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
12151052 101596 42 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2c(-c3ccccc3)cc3ccccc3c2-c2c(c(-c3ccccc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL1554297 101596 42 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2c(-c3ccccc3)cc3ccccc3c2-c2c(c(-c3ccccc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168271529 373226 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2cnccn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5173395 373226 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2cnccn2)cc1 10.1021/acs.jmedchem.2c00804
156499906 467331 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2cccc(C(F)(F)F)c2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6174115 467331 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2cccc(C(F)(F)F)c2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
23110764 390258 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 432 4 1 3 7.4 CCCc1cc2ccccc2c2c1OP(=O)(O)Oc1c(CCC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
CHEMBL5523382 390258 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 432 4 1 3 7.4 CCCc1cc2ccccc2c2c1OP(=O)(O)Oc1c(CCC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
169561564 389754 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 498 5 1 5 7.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC12CC3CC(C)(CC(C)(C3)C1)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499439 389754 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 498 5 1 5 7.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC12CC3CC(C)(CC(C)(C3)C1)C2 10.1021/acs.jmedchem.3c00053
71616529 271347 0 None -36 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None -36 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
178320777 467266 0 None 34 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172370 467266 0 None 34 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
169561599 389737 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 406 8 1 5 6.0 CCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499289 389737 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 406 8 1 5 6.0 CCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
178323826 467342 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 413 7 1 5 5.2 Oc1cc(CCOc2ccc(Cl)c3ccccc23)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6174286 467342 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 413 7 1 5 5.2 Oc1cc(CCOc2ccc(Cl)c3ccccc23)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
13892 8446 3 None -43 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499897 8446 3 None -43 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
CHEMBL6161601 8446 3 None -43 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
177646368 390881 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2cc(-c3ccccc3)c3ccccc3c2-c2c(cc(-c3ccccc3)c3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5559487 390881 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2cc(-c3ccccc3)c3ccccc3c2-c2c(cc(-c3ccccc3)c3ccccc23)O1 10.1021/acs.jmedchem.4c00359
156500025 467360 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174631 467360 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
169561626 389760 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cccc2ccccc12 10.1021/acs.jmedchem.3c00053
CHEMBL5499502 389760 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cccc2ccccc12 10.1021/acs.jmedchem.3c00053
169561711 389749 0 None None None Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 418 5 1 5 6.1 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCC1 10.1021/acs.jmedchem.3c00053
CHEMBL5499371 389749 0 None None None Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 418 5 1 5 6.1 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCC1 10.1021/acs.jmedchem.3c00053
177646597 390596 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1019 17 2 11 13.6 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5554981 390596 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1019 17 2 11 13.6 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
156499911 467398 0 None -23 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
CHEMBL6175294 467398 0 None -23 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
71616529 271347 0 None 36 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
71616526 271952 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3717743 271952 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
168271726 373501 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2cccnn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5177839 373501 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2cccnn2)cc1 10.1021/acs.jmedchem.2c00804
168275049 373508 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 450 7 3 6 3.4 O=C(NCCO)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5177947 373508 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 450 7 3 6 3.4 O=C(NCCO)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
168296983 375337 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccnnc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5206204 375337 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccnnc2)cc1 10.1021/acs.jmedchem.2c00804
71616529 271347 0 None -36 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None -36 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
146842444 385524 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 482 4 1 5 7.7 O=P(O)(OC1=Cc2ccccc2Oc2ccccc21)OC1=Cc2ccccc2Oc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222551 385524 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 482 4 1 5 7.7 O=P(O)(OC1=Cc2ccccc2Oc2ccccc21)OC1=Cc2ccccc2Oc2ccccc21 10.1021/acs.jmedchem.1c01813
169561646 389741 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499337 389741 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
168294481 375232 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 3 5.6 Fc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5204521 375232 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 3 5.6 Fc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c00804
178309794 467451 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176329 467451 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
178317355 466388 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6144284 466388 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OC[C@H]3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
162656514 354781 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 364 6 0 6 2.9 COc1ccc2c(c1)CCn1c-2cc(OCCOc2ccccc2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL4757870 354781 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 364 6 0 6 2.9 COc1ccc2c(c1)CCn1c-2cc(OCCOc2ccccc2)nc1=O 10.1021/acs.jmedchem.0c00272
1782609 366551 7 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 364 5 0 6 3.1 COc1cc2c(cc1OC)-c1cc(OCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4795786 366551 7 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 364 5 0 6 3.1 COc1cc2c(cc1OC)-c1cc(OCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
153309828 385400 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 450 4 1 3 7.9 O=P(O)(Oc1cc2ccccc2c2ccccc12)Oc1cc2ccccc2c2ccccc12 10.1021/acs.jmedchem.1c01813
CHEMBL5221836 385400 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 450 4 1 3 7.9 O=P(O)(Oc1cc2ccccc2c2ccccc12)Oc1cc2ccccc2c2ccccc12 10.1021/acs.jmedchem.1c01813
156499923 467406 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 334 11 2 4 5.1 CCCCCCCCCc1cc(O)cc(NCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6175417 467406 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 334 11 2 4 5.1 CCCCCCCCCc1cc(O)cc(NCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
168297446 375399 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 7 3 5 3.5 NC(=O)CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5207339 375399 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 7 3 5 3.5 NC(=O)CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
153309768 385373 0 None 11 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.4c00359
CHEMBL5221639 385373 0 None 11 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.4c00359
168278894 374072 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4ccncc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5186601 374072 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4ccncc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
153309803 385541 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2ccc(F)cc21)OC1=Cc2ccccc2Sc2ccc(F)cc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222655 385541 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2ccc(F)cc21)OC1=Cc2ccccc2Sc2ccc(F)cc21 10.1021/acs.jmedchem.1c01813
10171 3702 28 None -125 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
71616860 3702 28 None -125 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
CHEMBL3716365 3702 28 None -125 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
DB15346 3702 28 None -125 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
169561507 389820 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 442 4 1 4 7.0 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499895 389820 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 442 4 1 4 7.0 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
177646566 390564 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1095 22 2 14 12.1 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5550024 390564 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1095 22 2 14 12.1 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
89645365 271425 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715918 271425 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
178307663 467102 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 343 7 1 5 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6168786 467102 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 343 7 1 5 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
156500013 467404 0 None 35 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175409 467404 0 None 35 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
168289426 374395 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 392 5 2 4 4.8 OCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5191540 374395 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 392 5 2 4 4.8 OCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561499 389674 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCC1C 10.1021/acs.jmedchem.3c00053
CHEMBL5498791 389674 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCC1C 10.1021/acs.jmedchem.3c00053
178320777 467266 0 None 34 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172370 467266 0 None 34 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
153309791 385470 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1ccc2c(c1)Sc1c(OC)cccc1C(OP(=O)(O)OC1=Cc3ccc(OC)cc3Sc3c(OC)cccc31)=C2 10.1021/acs.jmedchem.1c01813
CHEMBL5222239 385470 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1ccc2c(c1)Sc1c(OC)cccc1C(OP(=O)(O)OC1=Cc3ccc(OC)cc3Sc3c(OC)cccc31)=C2 10.1021/acs.jmedchem.1c01813
168286764 374742 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5196547 374742 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
12151053 390157 36 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517998 390157 36 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
156499851 467333 0 None 37 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174163 467333 0 None 37 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168288253 374373 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 430 4 1 3 6.6 Clc1ccccc1-c1nnc(Cc2c[nH]c3ccccc23)nc1-c1ccccc1Cl 10.1021/acs.jmedchem.2c00804
CHEMBL5191278 374373 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 430 4 1 3 6.6 Clc1ccccc1-c1nnc(Cc2c[nH]c3ccccc23)nc1-c1ccccc1Cl 10.1021/acs.jmedchem.2c00804
153309826 385415 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1ccc(F)cc1C=C2OP(=O)(O)OC1=Cc2cc(F)ccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221914 385415 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1ccc(F)cc1C=C2OP(=O)(O)OC1=Cc2cc(F)ccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
156499983 467481 0 None 14 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6176923 467481 0 None 14 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
168274255 373588 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 469 7 2 5 4.3 CS(=O)(=O)NCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5179309 373588 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 469 7 2 5 4.3 CS(=O)(=O)NCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156499939 467006 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 4.3 CCCc1ccc(OCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6166272 467006 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 4.3 CCCc1ccc(OCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
153309853 373026 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 510 4 1 3 8.7 O=P(O)(CC1=Cc2ccccc2Sc2ccccc21)CC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5169963 373026 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 510 4 1 3 8.7 O=P(O)(CC1=Cc2ccccc2Sc2ccccc21)CC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
169561613 389693 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 12 1 5 7.5 CCCCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498892 389693 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 12 1 5 7.5 CCCCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
177646652 390859 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 975 15 2 10 13.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5559009 390859 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 975 15 2 10 13.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
162672947 366556 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 322 3 0 4 3.2 O=c1nc(OCc2ccccc2F)cc2n1CCc1ccccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL4795874 366556 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 322 3 0 4 3.2 O=c1nc(OCc2ccccc2F)cc2n1CCc1ccccc1-2 10.1021/acs.jmedchem.0c00272
169561620 389778 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 468 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc(C(C)C)ccc1C 10.1021/acs.jmedchem.3c00053
CHEMBL5499611 389778 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 468 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc(C(C)C)ccc1C 10.1021/acs.jmedchem.3c00053
101543344 390644 1 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 512 2 1 5 9.0 O=P1(O)Oc2c(-c3ccsc3)cc3ccccc3c2-c2c(c(-c3ccsc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5555830 390644 1 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 512 2 1 5 9.0 O=P1(O)Oc2c(-c3ccsc3)cc3ccccc3c2-c2c(c(-c3ccsc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
10171 3702 28 None 125 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
71616860 3702 28 None 125 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
CHEMBL3716365 3702 28 None 125 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
DB15346 3702 28 None 125 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.4c02335
168276448 373235 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccn2)nc1 10.1021/acs.jmedchem.2c00804
CHEMBL5173507 373235 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccn2)nc1 10.1021/acs.jmedchem.2c00804
168275915 373559 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2cccnn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5178841 373559 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2cccnn2)cc1 10.1021/acs.jmedchem.2c00804
168289877 374439 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 463 8 2 5 4.7 COCCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5192235 374439 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 463 8 2 5 4.7 COCCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
23628846 389939 33 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 652 4 1 3 12.2 O=P1(O)Oc2c(-c3ccc(-c4ccccc4)cc3)cc3ccccc3c2-c2c(c(-c3ccc(-c4ccccc4)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5505750 389939 33 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 652 4 1 3 12.2 O=P1(O)Oc2c(-c3ccc(-c4ccccc4)cc3)cc3ccccc3c2-c2c(c(-c3ccc(-c4ccccc4)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168289213 374571 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 502 5 1 5 4.2 CN1CCN(C(=O)c2ccc(-c3nnc(Cc4c[nH]c5ccccc45)nc3-c3ccccc3)cc2)CC1=O 10.1021/acs.jmedchem.2c00804
CHEMBL5193904 374571 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 502 5 1 5 4.2 CN1CCN(C(=O)c2ccc(-c3nnc(Cc4c[nH]c5ccccc45)nc3-c3ccccc3)cc2)CC1=O 10.1021/acs.jmedchem.2c00804
177374259 390495 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5542801 390495 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
168283011 373950 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 6 1 4 5.3 CN(C)Cc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5184825 373950 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 6 1 4 5.3 CN(C)Cc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
1785231 354144 7 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 358 8 0 6 3.4 CCCCCCOc1cc2n(c(=O)n1)CCc1cc(OC)c(OC)cc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL4750532 354144 7 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 358 8 0 6 3.4 CCCCCCOc1cc2n(c(=O)n1)CCc1cc(OC)c(OC)cc1-2 10.1021/acs.jmedchem.0c00272
71616529 271347 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
13892 8446 3 None 43 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499897 8446 3 None 43 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
CHEMBL6161601 8446 3 None 43 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
71616971 272243 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3718710 272243 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 415 4 0 7 2.8 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
169561594 389682 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 420 5 1 6 5.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCOCC1 10.1021/acs.jmedchem.3c00053
CHEMBL5498849 389682 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 420 5 1 6 5.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCOCC1 10.1021/acs.jmedchem.3c00053
168274538 373384 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 478 6 1 7 4.9 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(C(=O)OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5175765 373384 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 478 6 1 7 4.9 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(C(=O)OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
168277900 373754 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 423 6 1 6 4.7 COc1ccc(-c2nnc(Cc3n[nH]c4ccccc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5181719 373754 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 423 6 1 6 4.7 COc1ccc(-c2nnc(Cc3n[nH]c4ccccc34)nc2-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.2c00804
156499989 467226 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.7 CCCc1ccc(CCc2cc(O)cc(OCC3OCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6171578 467226 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.7 CCCc1ccc(CCc2cc(O)cc(OCC3OCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
169561623 389839 0 None None None Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 452 11 1 7 4.8 CCOCCOCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5500007 389839 0 None None None Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 452 11 1 7 4.8 CCOCCOCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
177646674 390788 0 None None None Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 750 2 1 3 13.7 O=P1(O)Oc2c(C3=C4C=CC=C5C=CC6=C(C(=C3)CC=C6)C54)cc3ccccc3c2-c2c(c(-c3cc4cccc5ccc6cccc3c6c54)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5558092 390788 0 None None None Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 750 2 1 3 13.7 O=P1(O)Oc2c(C3=C4C=CC=C5C=CC6=C(C(=C3)CC=C6)C54)cc3ccccc3c2-c2c(c(-c3cc4cccc5ccc6cccc3c6c54)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
169561640 389761 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 10 1 4 7.2 CCCCCCCCP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499506 389761 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 10 1 4 7.2 CCCCCCCCP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
71616165 271803 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 10.1021/acs.jmedchem.0c00272
CHEMBL3717201 271803 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 471 6 0 7 2.7 CN(CC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O)Cc1ccccc1 10.1021/acs.jmedchem.0c00272
162656095 354595 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 393 4 0 8 2.1 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL4755764 354595 0 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 393 4 0 8 2.1 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
71616529 271347 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
156542972 385322 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 502 4 1 3 8.5 O=P(O)(O/C1=C/c2ccccc2/C=C\c2ccccc21)O/C1=C/c2ccccc2/C=C\c2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221312 385322 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 502 4 1 3 8.5 O=P(O)(O/C1=C/c2ccccc2/C=C\c2ccccc21)O/C1=C/c2ccccc2/C=C\c2ccccc21 10.1021/acs.jmedchem.1c01813
168272726 373580 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 380 4 1 3 5.4 Fc1ccc2c(Cc3nnc(-c4ccccc4)c(-c4ccccc4)n3)c[nH]c2c1 10.1021/acs.jmedchem.2c00804
CHEMBL5179128 373580 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 380 4 1 3 5.4 Fc1ccc2c(Cc3nnc(-c4ccccc4)c(-c4ccccc4)n3)c[nH]c2c1 10.1021/acs.jmedchem.2c00804
149484987 390125 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 586 4 1 5 9.0 CN(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(N(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517642 390125 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 586 4 1 5 9.0 CN(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(N(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
168292424 375087 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccncc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5202315 375087 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccncc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
172464263 389812 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 512 5 1 5 8.2 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc2ccccc2c2ccccc12 10.1021/acs.jmedchem.3c00053
CHEMBL5499845 389812 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 512 5 1 5 8.2 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc2ccccc2c2ccccc12 10.1021/acs.jmedchem.3c00053
156499851 467333 0 None 37 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174163 467333 0 None 37 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168279722 374223 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 374 4 1 5 5.4 c1csc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2cccs2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5188586 374223 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 374 4 1 5 5.4 c1csc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2cccs2)c1 10.1021/acs.jmedchem.2c00804
153309772 385420 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2cc(F)ccc21)OC1=Cc2ccccc2Sc2cc(F)ccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221939 385420 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2cc(F)ccc21)OC1=Cc2ccccc2Sc2cc(F)ccc21 10.1021/acs.jmedchem.1c01813
169561569 389685 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 476 4 1 4 7.7 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498853 389685 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 476 4 1 4 7.7 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
168282518 373902 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 469 7 2 5 4.3 CS(=O)(=O)NCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5183982 373902 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 469 7 2 5 4.3 CS(=O)(=O)NCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
177657948 390812 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1418 45 2 21 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5558350 390812 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1418 45 2 21 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
156500033 467452 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176351 467452 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 2.8 CCOc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
169561643 389643 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C(C)(C)[C@H]2CC[C@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5498557 389643 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C(C)(C)[C@H]2CC[C@]1(C)C2 10.1021/acs.jmedchem.3c00053
71616166 271986 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 424 5 1 7 2.0 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3717853 271986 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 424 5 1 7 2.0 CC(C)CC(O)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
71616529 271347 0 None 36 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
168297380 375338 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 518 4 1 3 6.8 Brc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(Br)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5206221 375338 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 518 4 1 3 6.8 Brc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(Br)cc2)cc1 10.1021/acs.jmedchem.2c00804
153027899 385539 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1ccc2c(c1)Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2cc(OC)ccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222633 385539 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1ccc2c(c1)Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2cc(OC)ccc21 10.1021/acs.jmedchem.1c01813
156499886 467445 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 369 9 1 4 4.9 CCCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176292 467445 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 369 9 1 4 4.9 CCCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
178310829 467494 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 313 6 1 4 3.5 Oc1cc(CCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6177171 467494 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 313 6 1 4 3.5 Oc1cc(CCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
162677233 366832 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 382 5 0 6 3.2 COc1cc2c(cc1OC)-c1cc(OCc3ccccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4799579 366832 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 382 5 0 6 3.2 COc1cc2c(cc1OC)-c1cc(OCc3ccccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
16050033 390144 34 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3cccc4ccccc34)cc3ccccc3c2-c2c(c(-c3cccc4ccccc34)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5517888 390144 34 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3cccc4ccccc34)cc3ccccc3c2-c2c(c(-c3cccc4ccccc34)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168270713 373031 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 370 4 1 4 4.5 FC(F)(F)Oc1ccccc1-c1cnc(Cc2c[nH]c3ccccc23)nn1 10.1021/acs.jmedchem.2c00804
CHEMBL5170018 373031 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 370 4 1 4 4.5 FC(F)(F)Oc1ccccc1-c1cnc(Cc2c[nH]c3ccccc23)nn1 10.1021/acs.jmedchem.2c00804
71616642 271855 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3717416 271855 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 412 6 0 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(COC3CCCC3)ccc1-2 10.1021/acs.jmedchem.0c00272
153309743 385302 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2c(F)cccc2Sc2ccccc21)OC1=Cc2c(F)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221157 385302 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2c(F)cccc2Sc2ccccc21)OC1=Cc2c(F)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
71598639 272433 31 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU induced intracellular cAMP production pretreated for 15 mins followed by forskolin and agonist addition and measured after 30 mins by HitHunter luminescence based microplate reader assayAntagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU induced intracellular cAMP production pretreated for 15 mins followed by forskolin and agonist addition and measured after 30 mins by HitHunter luminescence based microplate reader assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.1c01813
CHEMBL3719364 272433 31 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU induced intracellular cAMP production pretreated for 15 mins followed by forskolin and agonist addition and measured after 30 mins by HitHunter luminescence based microplate reader assayAntagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU induced intracellular cAMP production pretreated for 15 mins followed by forskolin and agonist addition and measured after 30 mins by HitHunter luminescence based microplate reader assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.1c01813
71598639 272433 31 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU-induced inhibition of forskolin stimulated cAMP production preincubated for 15 mins followed by forskolin and 6-OAU stimulation and measured after 30 mins by luminescence methodAntagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU-induced inhibition of forskolin stimulated cAMP production preincubated for 15 mins followed by forskolin and 6-OAU stimulation and measured after 30 mins by luminescence method
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3719364 272433 31 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU-induced inhibition of forskolin stimulated cAMP production preincubated for 15 mins followed by forskolin and 6-OAU stimulation and measured after 30 mins by luminescence methodAntagonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in 6-OAU-induced inhibition of forskolin stimulated cAMP production preincubated for 15 mins followed by forskolin and 6-OAU stimulation and measured after 30 mins by luminescence method
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c01378
168286688 374669 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ncccn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5195413 374669 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 5 4.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ncccn2)cc1 10.1021/acs.jmedchem.2c00804
168269632 373122 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL5171669 373122 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.4c02335
153309755 385300 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 506 4 1 3 7.7 O=P(O)(O/C1=C/c2ccccc2CCc2ccccc21)O/C1=C/c2ccccc2CCc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221144 385300 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 506 4 1 3 7.7 O=P(O)(O/C1=C/c2ccccc2CCc2ccccc21)O/C1=C/c2ccccc2CCc2ccccc21 10.1021/acs.jmedchem.1c01813
153309768 385373 0 None -11 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None -11 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
76684891 271824 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 436 6 1 8 2.1 O=C(O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3717307 271824 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 436 6 1 8 2.1 O=C(O)COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
156500127 467062 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 8 1 5 4.1 CCCc1ccc(CCc2cc(O)cc(OCC3OCCC(C)O3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6167776 467062 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 8 1 5 4.1 CCCc1ccc(CCc2cc(O)cc(OCC3OCCC(C)O3)n2)cc1 10.1021/acs.jmedchem.4c02335
148279656 385394 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2cccc(F)c2Sc2ccccc21)OC1=Cc2cccc(F)c2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221762 385394 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2cccc(F)c2Sc2ccccc21)OC1=Cc2cccc(F)c2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
15948415 389945 35 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3ccc4ccccc4c3)cc3ccccc3c2-c2c(c(-c3ccc4ccccc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5505825 389945 35 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3ccc4ccccc4c3)cc3ccccc3c2-c2c(c(-c3ccc4ccccc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
71616526 271952 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3717743 271952 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of decanoic acid-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
168287473 374582 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5194077 374582 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
178321387 467250 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 363 6 1 5 4.3 Cc1cc(Cl)ccc1OCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6171982 467250 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 363 6 1 5 4.3 Cc1cc(Cl)ccc1OCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
169561560 389848 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 350 4 1 5 4.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC 10.1021/acs.jmedchem.3c00053
CHEMBL5500128 389848 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 350 4 1 5 4.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC 10.1021/acs.jmedchem.3c00053
156499885 466963 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.4 CCCc1ccc(COCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6165269 466963 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 9 1 5 4.4 CCCc1ccc(COCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
146294474 390044 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 480 2 1 5 8.1 O=P1(O)Oc2c(-c3ccoc3)cc3ccccc3c2-c2c(c(-c3ccoc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5512562 390044 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 480 2 1 5 8.1 O=P1(O)Oc2c(-c3ccoc3)cc3ccccc3c2-c2c(c(-c3ccoc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168278353 374231 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 476 8 2 5 4.6 CN(C)CCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5188700 374231 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 476 8 2 5 4.6 CN(C)CCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
177646105 390364 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 977 14 2 11 12.4 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5532207 390364 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 977 14 2 11 12.4 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
172458717 389767 0 None None None Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 370 4 1 3 5.6 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499543 389767 0 None None None Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 370 4 1 3 5.6 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)O[C@@H]1C(C)(C)[C@@H]2CC[C@@]1(C)C2 10.1021/acs.jmedchem.3c00053
169561501 389739 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCC(C)C1 10.1021/acs.jmedchem.3c00053
CHEMBL5499314 389739 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCC(C)C1 10.1021/acs.jmedchem.3c00053
101849670 390273 2 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1cccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4cccc(OC)c4)cc4ccccc4c2-3)c1 10.1021/acs.jmedchem.4c00359
CHEMBL5523561 390273 2 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1cccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4cccc(OC)c4)cc4ccccc4c2-3)c1 10.1021/acs.jmedchem.4c00359
168269632 373122 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL5171669 373122 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.4c02335
168271424 373684 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 461 6 1 5 5.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5180699 373684 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 461 6 1 5 5.1 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
24894958 390039 34 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 612 2 1 3 11.5 CC(C)(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(C)(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5512456 390039 34 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 612 2 1 3 11.5 CC(C)(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(C)(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
153309761 385503 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccc(F)cc2Sc2ccccc21)OC1=Cc2ccc(F)cc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222449 385503 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccc(F)cc2Sc2ccccc21)OC1=Cc2ccc(F)cc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
76684484 271745 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 328 4 0 6 2.0 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3717000 271745 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 328 4 0 6 2.0 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
156499911 467398 0 None 23 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
CHEMBL6175294 467398 0 None 23 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at human GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 358 8 1 6 3.3 CCOc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cn1 10.1021/acs.jmedchem.4c02335
177646141 390164 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1271 34 2 18 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5518112 390164 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1271 34 2 18 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
71616529 271347 0 None -36 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None -36 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated mouse RAW 264.7 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
178306152 466932 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 363 6 1 5 4.3 Cc1cc(OCc2cc(O)cc(OCC3CCCCO3)n2)ccc1Cl 10.1021/acs.jmedchem.4c02335
CHEMBL6164425 466932 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 363 6 1 5 4.3 Cc1cc(OCc2cc(O)cc(OCC3CCCCO3)n2)ccc1Cl 10.1021/acs.jmedchem.4c02335
153309834 385537 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1c(F)cccc1C=C2OP(=O)(O)OC1=Cc2cccc(F)c2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222627 385537 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1c(F)cccc1C=C2OP(=O)(O)OC1=Cc2cccc(F)c2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
149043775 385506 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 630 8 1 7 10.0 CC(C)Oc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC(C)C)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222466 385506 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 630 8 1 7 10.0 CC(C)Oc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC(C)C)cccc21 10.1021/acs.jmedchem.1c01813
168278009 373268 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5173991 373268 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
168296821 375405 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 455 6 2 5 4.2 CNS(=O)(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5207475 375405 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 455 6 2 5 4.2 CNS(=O)(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
168269664 372985 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5169375 372985 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1cccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
169561591 389705 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 420 9 1 5 6.4 CCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498993 389705 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 420 9 1 5 6.4 CCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
153309832 385562 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2c(F)cccc21)OC1=Cc2ccccc2Sc2c(F)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222790 385562 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2ccccc2Sc2c(F)cccc21)OC1=Cc2ccccc2Sc2c(F)cccc21 10.1021/acs.jmedchem.1c01813
149469204 375057 0 None 4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5201755 375057 0 None 4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
13892 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499897 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
CHEMBL6161601 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
168288085 374724 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5196255 374724 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156499901 466788 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.6 CCCc1ccc(CCc2cc(O)cc(COC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6161204 466788 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 4.6 CCCc1ccc(CCc2cc(O)cc(COC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168038773 374217 3 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 339 5 1 5 4.2 c1ccc(-c2nnc(NCc3cccnc3)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5188398 374217 3 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 339 5 1 5 4.2 c1ccc(-c2nnc(NCc3cccnc3)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
13892 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
156499897 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
CHEMBL6161601 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 10.1021/acs.jmedchem.4c02335
168285407 374617 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 449 7 3 5 4.0 O=C(NCCO)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5194648 374617 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 449 7 3 5 4.0 O=C(NCCO)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561612 389798 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 470 5 1 5 6.8 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499742 389798 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 470 5 1 5 6.8 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.3c00053
826353 373053 2 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 235 0 0 2 4.2 N#CC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5170482 373053 2 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 235 0 0 2 4.2 N#CC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
156500013 467404 0 None 35 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175409 467404 0 None 35 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
153309776 385319 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1ccc2c(c1)C(OP(=O)(O)OC1=Cc3ccccc3Sc3ccc(OC)cc31)=Cc1ccccc1S2 10.1021/acs.jmedchem.1c01813
CHEMBL5221258 385319 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1ccc2c(c1)C(OP(=O)(O)OC1=Cc3ccccc3Sc3ccc(OC)cc31)=Cc1ccccc1S2 10.1021/acs.jmedchem.1c01813
162658448 355008 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 383 5 0 7 2.6 COc1cc2c(cc1OC)-c1cc(OCc3ncccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4760776 355008 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 383 5 0 7 2.6 COc1cc2c(cc1OC)-c1cc(OCc3ncccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
156500013 467404 0 None 35 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175409 467404 0 None 35 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 381 6 1 4 4.5 Oc1cc(CCc2ccc(C(F)(F)F)cc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
156499964 467461 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 369 8 1 4 4.7 CC(C)Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176562 467461 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 369 8 1 4 4.7 CC(C)Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
99589 390841 70 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5558714 390841 70 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168280183 373914 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 0 5 4.4 c1ccc(-c2nnc(Cc3cnc4ccccn34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5184294 373914 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 0 5 4.4 c1ccc(-c2nnc(Cc3cnc4ccccn34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
153309814 385399 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1cccc2c1Sc1c(OC)cccc1C(OP(=O)(O)OC1=Cc3cccc(OC)c3Sc3c(OC)cccc31)=C2 10.1021/acs.jmedchem.1c01813
CHEMBL5221808 385399 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1cccc2c1Sc1c(OC)cccc1C(OP(=O)(O)OC1=Cc3cccc(OC)c3Sc3c(OC)cccc31)=C2 10.1021/acs.jmedchem.1c01813
153309795 385472 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1ccc2c(c1)Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2cc(C)ccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222247 385472 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1ccc2c(c1)Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2cc(C)ccc21 10.1021/acs.jmedchem.1c01813
149016467 385379 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 450 4 1 3 7.9 O=P(O)(Oc1c2ccccc2cc2ccccc12)Oc1c2ccccc2cc2ccccc12 10.1021/acs.jmedchem.1c01813
CHEMBL5221657 385379 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 450 4 1 3 7.9 O=P(O)(Oc1c2ccccc2cc2ccccc12)Oc1c2ccccc2cc2ccccc12 10.1021/acs.jmedchem.1c01813
162656291 354808 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 358 5 0 7 2.0 COc1cc2c(cc1OC)-c1cc(OCC3CCCO3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4758226 354808 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 358 5 0 7 2.0 COc1cc2c(cc1OC)-c1cc(OCC3CCCO3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
169561714 389715 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 412 5 1 5 5.9 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1ccccc1 10.1021/acs.jmedchem.3c00053
CHEMBL5499064 389715 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 412 5 1 5 5.9 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1ccccc1 10.1021/acs.jmedchem.3c00053
49839941 390038 19 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 536 2 1 3 9.1 O=P1(O)Oc2c(-c3ccc(F)cc3)cc3ccccc3c2-c2c(c(-c3ccc(F)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5512452 390038 19 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 536 2 1 3 9.1 O=P1(O)Oc2c(-c3ccc(F)cc3)cc3ccccc3c2-c2c(c(-c3ccc(F)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
89645206 271583 0 None -50 2 Mouse 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassayInverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3716446 271583 0 None -50 2 Mouse 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassayInverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
146294464 390128 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 580 2 1 5 10.4 O=P1(O)Oc2c(-c3ccc4occc4c3)cc3ccccc3c2-c2c(c(-c3ccc4occc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5517684 390128 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 580 2 1 5 10.4 O=P1(O)Oc2c(-c3ccc4occc4c3)cc3ccccc3c2-c2c(c(-c3ccc4occc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
44517926 390557 30 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 568 2 1 3 10.2 O=P1(O)Oc2c(-c3ccc(Cl)cc3)cc3ccccc3c2-c2c(c(-c3ccc(Cl)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5549894 390557 30 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 568 2 1 3 10.2 O=P1(O)Oc2c(-c3ccc(Cl)cc3)cc3ccccc3c2-c2c(c(-c3ccc(Cl)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
169561561 389844 0 None None None Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 376 5 1 5 5.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CC1 10.1021/acs.jmedchem.3c00053
CHEMBL5500059 389844 0 None None None Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 376 5 1 5 5.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CC1 10.1021/acs.jmedchem.3c00053
169561727 389786 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 430 5 1 5 6.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H]2CC[C@H]1C2 10.1021/acs.jmedchem.3c00053
CHEMBL5499646 389786 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 430 5 1 5 6.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H]2CC[C@H]1C2 10.1021/acs.jmedchem.3c00053
177645859 390130 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1065 21 2 13 12.1 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5517721 390130 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1065 21 2 13 12.1 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
168285211 374782 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5197127 374782 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
169561589 389681 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 406 5 1 6 4.6 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCOC1 10.1021/acs.jmedchem.3c00053
CHEMBL5498845 389681 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 406 5 1 6 4.6 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCOC1 10.1021/acs.jmedchem.3c00053
153309787 385572 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1cccc(F)c1C=C2OP(=O)(O)OC1=Cc2c(F)cccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222848 385572 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1cccc(F)c1C=C2OP(=O)(O)OC1=Cc2c(F)cccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
168268962 373040 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 6 1 6 4.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5170226 373040 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 6 1 6 4.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
71616529 271347 0 None 36 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at GPR84 in LPS-treated human THP-1 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
102147274 390487 2 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccccc1-c1cc2ccccc2c2c1OP(=O)(O)Oc1c(-c3ccccc3OC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
CHEMBL5542707 390487 2 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccccc1-c1cc2ccccc2c2c1OP(=O)(O)Oc1c(-c3ccccc3OC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
169561503 389759 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCC(C)CC1 10.1021/acs.jmedchem.3c00053
CHEMBL5499499 389759 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.4 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCC(C)CC1 10.1021/acs.jmedchem.3c00053
153309749 385502 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2cccc(Cl)c2Sc2ccccc21)OC1=Cc2cccc(Cl)c2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222448 385502 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2cccc(Cl)c2Sc2ccccc21)OC1=Cc2cccc(Cl)c2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
172461593 389793 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 460 6 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1CCCC[C@@H]1C(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5499700 389793 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 460 6 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1CCCC[C@@H]1C(C)C 10.1021/acs.jmedchem.3c00053
168272643 373504 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 455 6 2 5 4.2 CNS(=O)(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5177895 373504 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 455 6 2 5 4.2 CNS(=O)(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561629 389818 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C[C@@H]2CC[C@@]1(C)C2(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5499870 389818 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C[C@@H]2CC[C@@]1(C)C2(C)C 10.1021/acs.jmedchem.3c00053
153309809 385466 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2cc(F)ccc2Sc2ccccc21)OC1=Cc2cc(F)ccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222219 385466 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 550 4 1 5 8.7 O=P(O)(OC1=Cc2cc(F)ccc2Sc2ccccc21)OC1=Cc2cc(F)ccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
149469204 375057 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5201755 375057 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
156499916 466928 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 349 11 1 4 5.4 CCCCCCCCCc1cc(O)cc(OCC2CCCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6164354 466928 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 349 11 1 4 5.4 CCCCCCCCCc1cc(O)cc(OCC2CCCCCO2)n1 10.1021/acs.jmedchem.4c02335
156499902 467432 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 5.1 CCCCCc1ccc(-c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6176041 467432 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 355 8 1 4 5.1 CCCCCc1ccc(-c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168269754 373126 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 294 4 1 3 4.2 CC(C)c1nnc(Cc2c[nH]c3ccccc23)nc1C(C)C 10.1021/acs.jmedchem.2c00804
CHEMBL5171681 373126 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 294 4 1 3 4.2 CC(C)c1nnc(Cc2c[nH]c3ccccc23)nc1C(C)C 10.1021/acs.jmedchem.2c00804
168285639 374899 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2cnccn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5199072 374899 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2cnccn2)cc1 10.1021/acs.jmedchem.2c00804
44517926 390557 30 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 568 2 1 3 10.2 O=P1(O)Oc2c(-c3ccc(Cl)cc3)cc3ccccc3c2-c2c(c(-c3ccc(Cl)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5549894 390557 30 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 568 2 1 3 10.2 O=P1(O)Oc2c(-c3ccc(Cl)cc3)cc3ccccc3c2-c2c(c(-c3ccc(Cl)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168291546 375033 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 4.5 COC(=O)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5201371 375033 0 None None None Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 4.5 COC(=O)c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
86688463 272162 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 344 4 0 7 1.3 COc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3718436 272162 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 344 4 0 7 1.3 COc1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
178323850 467460 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 3.4 COc1cccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6176540 467460 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 359 8 1 6 3.4 COc1cccc(OCCc2cc(O)cc(OCC3CCCCO3)n2)c1 10.1021/acs.jmedchem.4c02335
15948415 389945 35 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3ccc4ccccc4c3)cc3ccccc3c2-c2c(c(-c3ccc4ccccc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5505825 389945 35 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3ccc4ccccc4c3)cc3ccccc3c2-c2c(c(-c3ccc4ccccc4c3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
168294247 375296 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccncc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5205576 375296 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccncc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156500025 467360 0 None -17 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174631 467360 0 None -17 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
12151053 390157 36 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517998 390157 36 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
147694370 385422 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 530 4 1 3 8.3 O=P(O)(OC1=Cc2ccccc2C2(CC2)c2ccccc21)OC1=Cc2ccccc2C2(CC2)c2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221949 385422 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 530 4 1 3 8.3 O=P(O)(OC1=Cc2ccccc2C2(CC2)c2ccccc21)OC1=Cc2ccccc2C2(CC2)c2ccccc21 10.1021/acs.jmedchem.1c01813
169561508 389659 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 444 8 1 5 6.4 CCCCCC#CCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498677 389659 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 444 8 1 5 6.4 CCCCCC#CCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
149469204 375057 0 None -4 2 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5201755 375057 0 None -4 2 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at mouse GPR84 expressed in HEK293 cells assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
177639578 390126 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1241 33 2 17 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5517647 390126 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1241 33 2 17 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
153309778 385501 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 602 8 1 7 9.2 CCOc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OCC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222438 385501 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 602 8 1 7 9.2 CCOc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OCC)cccc21 10.1021/acs.jmedchem.1c01813
156499869 467252 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172099 467252 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
71617557 271412 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 314 3 0 6 1.3 O=c1nc(OCC2COCCO2)cc2n1CCc1ccccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3715879 271412 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 314 3 0 6 1.3 O=c1nc(OCC2COCCO2)cc2n1CCc1ccccc1-2 10.1021/acs.jmedchem.0c00272
156500043 466966 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 8 1 5 3.9 CCCc1ccc(CCc2cc(O)cc(OCC3OCC(C)CO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6165391 466966 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 371 8 1 5 3.9 CCCc1ccc(CCc2cc(O)cc(OCC3OCC(C)CO3)n2)cc1 10.1021/acs.jmedchem.4c02335
178321074 467267 0 None None None Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 287 5 1 5 2.9 CCCc1cc(O)cc(OCC2Oc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6172440 467267 0 None None None Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 287 5 1 5 2.9 CCCc1cc(O)cc(OCC2Oc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
156499869 467252 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172099 467252 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 341 7 1 4 4.1 CCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168292609 375088 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
CHEMBL5202325 375088 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1cccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)c1 10.1021/acs.jmedchem.2c00804
156499983 467481 0 None -14 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6176923 467481 0 None -14 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
146294470 390555 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 616 4 1 7 8.4 COC(=O)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(=O)OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5549864 390555 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 616 4 1 7 8.4 COC(=O)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(=O)OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
156500025 467360 0 None 17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174631 467360 0 None 17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168289914 374594 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5194322 374594 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 1 5 5.1 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
99589 390841 70 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5558714 390841 70 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
156500025 467360 0 None 17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174631 467360 0 None 17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 357 8 1 5 3.3 CCCc1ccc(CCc2cc(O)cc(OCC3COCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
11812376 390385 0 None None None Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 448 0 1 3 7.8 O=P1(O)Oc2c(c3ccccc3c3ccccc23)-c2c(c3ccccc3c3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5532478 390385 0 None None None Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 448 0 1 3 7.8 O=P1(O)Oc2c(c3ccccc3c3ccccc23)-c2c(c3ccccc3c3ccccc23)O1 10.1021/acs.jmedchem.4c00359
162672882 366468 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 440 8 0 7 3.5 O=c1nc(OCCOc2cnccn2)cc2n1CCc1cc(CCc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL4794652 366468 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 440 8 0 7 3.5 O=c1nc(OCCOc2cnccn2)cc2n1CCc1cc(CCc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c00272
168281800 374047 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 434 6 1 5 5.3 CC(=O)OCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5186088 374047 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 434 6 1 5 5.3 CC(=O)OCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
164887573 373694 13 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 461 6 1 5 5.1 c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5180818 373694 13 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 461 6 1 5 5.1 c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
75203411 271139 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 392 4 0 7 2.7 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3714917 271139 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 392 4 0 7 2.7 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
90253074 271104 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 533 6 0 9 2.7 CC(C)(Oc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)C(=O)N1CCOCC1 nan
CHEMBL3714778 271104 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 533 6 0 9 2.7 CC(C)(Oc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O)C(=O)N1CCOCC1 nan
90242304 271150 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 390 4 0 5 3.4 CC(C)C1CC(COc2cc3n(c(=O)n2)CCc2cc(C#CC4CC4)ccc2-3)O1 nan
CHEMBL3714950 271150 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 390 4 0 5 3.4 CC(C)C1CC(COc2cc3n(c(=O)n2)CCc2cc(C#CC4CC4)ccc2-3)O1 nan
76684580 271398 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 375 4 0 6 3.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 nan
CHEMBL3715834 271398 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 375 4 0 6 3.1 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3cccnc3)ccc1-2 nan
76684673 271665 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 5 1 6 3.4 O=C(O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
CHEMBL3716749 271665 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 418 5 1 6 3.4 O=C(O)c1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3CCCO3)nc2=O)c1 nan
90241698 271706 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 430 4 1 8 1.7 CNCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
CHEMBL3716896 271706 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 430 4 1 8 1.7 CNCC#Cc1ccc2c(c1)CCn1c-2cc(OCC2COc3ncccc3O2)nc1=O nan
90239911 271714 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 8 0 8 3.0 CN(C)CCCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
CHEMBL3716911 271714 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 463 8 0 8 3.0 CN(C)CCCOc1ccc2c(c1)CCn1c-2cc(OCC2COc3ccccc3O2)nc1=O nan
90242162 271716 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 399 4 0 6 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3716913 271716 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 399 4 0 6 3.6 N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
76684486 271961 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 376 4 0 6 2.9 COc1ccc2c(c1)CCn1c-2cc(OCC2Cc3ccccc3O2)nc1=O nan
CHEMBL3717778 271961 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 376 4 0 6 2.9 COc1ccc2c(c1)CCn1c-2cc(OCC2Cc3ccccc3O2)nc1=O nan
90242307 271984 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 395 6 0 8 2.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
CHEMBL3717849 271984 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 395 6 0 8 2.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3ncco3)ccc1-2 nan
76684574 272232 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 398 6 0 7 2.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3CCCO3)ccc1-2 nan
CHEMBL3718665 272232 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM HEPES at pH 7.4 by top-count assay
ChEMBL 398 6 0 7 2.6 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCC3CCCO3)ccc1-2 nan
76684773 271642 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 414 4 0 6 4.4 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccc(Cl)s3)ccc1-2 nan
CHEMBL3716645 271642 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 414 4 0 6 4.4 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3ccc(Cl)s3)ccc1-2 nan
76684771 271765 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 424 4 0 5 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3cccc4ccccc34)ccc1-2 nan
CHEMBL3717070 271765 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 424 4 0 5 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(-c3cccc4ccccc34)ccc1-2 nan
90242114 272086 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 378 3 0 5 3.4 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
CHEMBL3718208 272086 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 378 3 0 5 3.4 CC(C)(C)C#Cc1ccc2c(c1)CCn1c-2cc(OCC2CCCO2)nc1=O nan
90242623 272268 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 454 6 0 6 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc4ccccc34)ccc1-2 nan
CHEMBL3718784 272268 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes assessed as inhibition of 3,3'-di-indolylmethane-induced [35S]GTPgammaS binding treated for 90 mins after 3,3'-di-indolylmethane stimulation in buffer containing 20 mM Tris at pH 7.5 by top-count assay
ChEMBL 454 6 0 6 4.8 O=c1nc(OCC2CCCO2)cc2n1CCc1cc(OCc3cccc4ccccc34)ccc1-2 nan
89645856 271126 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 438 3 1 8 1.2 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3(O)CCOCC3)ccc1-2 nan
CHEMBL3714871 271126 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 438 3 1 8 1.2 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(C#CC3(O)CCOCC3)ccc1-2 nan
89645514 271474 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
CHEMBL3716099 271474 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 8 0 8 2.1 CC(C)OCCOc1ccc2c(c1)CCn1c-2cc(OC[C@H]2COCCO2)nc1=O nan
89645350 271515 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NCC3CCOCC3)ccc1-2 nan
CHEMBL3716225 271515 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 8 2.1 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(NCC3CCOCC3)ccc1-2 nan
71616970 271647 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 391 4 0 7 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccncc3)ccc1-2 nan
CHEMBL3716680 271647 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 391 4 0 7 2.3 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(-c3ccncc3)ccc1-2 nan
89645690 271661 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)ccc1F nan
CHEMBL3716729 271661 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 451 5 1 7 2.2 NC(=O)c1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)ccc1F nan
71617559 271694 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 4 0 8 2.2 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3716848 271694 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 4 0 8 2.2 N#Cc1ccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71616862 271746 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 7 0 8 1.8 CC1(COCc2ccc3c(c2)CCn2c-3cc(OC[C@@H]3COCCO3)nc2=O)COC1 nan
CHEMBL3717001 271746 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 428 7 0 8 1.8 CC1(COCc2ccc3c(c2)CCn2c-3cc(OC[C@@H]3COCCO3)nc2=O)COC1 nan
71617317 272006 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 4 1 7 1.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCCO)ccc1-2 nan
CHEMBL3717936 272006 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 382 4 1 7 1.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCCO)ccc1-2 nan
71616527 272046 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 3 0 8 1.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ncccn3)ccc1-2 nan
CHEMBL3718076 272046 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 416 3 0 8 1.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#Cc3ncccn3)ccc1-2 nan
71616289 272244 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 408 5 0 8 2.1 CCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
CHEMBL3718711 272244 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 408 5 0 8 2.1 CCn1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)cn1 nan
71616972 272270 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
CHEMBL3718792 272270 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 415 4 0 7 2.8 N#Cc1cccc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)c1 nan
89645640 272292 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 5 0 7 3.0 CN(c1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O)C1CCCCC1 nan
CHEMBL3718852 272292 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 425 5 0 7 3.0 CN(c1ccc2c(c1)CCn1c-2cc(OC[C@@H]2COCCO2)nc1=O)C1CCCCC1 nan
89645424 272365 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 0 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCCF)ccc1-2 nan
CHEMBL3719125 272365 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 0 7 1.6 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(OCCF)ccc1-2 nan
71617674 272370 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 405 4 0 7 2.6 Cc1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)ccn1 nan
CHEMBL3719139 272370 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assayAntagonist activity against GPR84 (unknown origin) expressed in cell membranes incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 405 4 0 7 2.6 Cc1cc(-c2ccc3c(c2)CCn2c-3cc(OCC3COCCO3)nc2=O)ccn1 nan
177646412 390635 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 502 6 1 3 8.9 O=P(O)(Oc1cc2ccccc2cc1-c1ccccc1)Oc1cc2ccccc2cc1-c1ccccc1 10.1021/acs.jmedchem.4c00359
CHEMBL5555671 390635 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 502 6 1 3 8.9 O=P(O)(Oc1cc2ccccc2cc1-c1ccccc1)Oc1cc2ccccc2cc1-c1ccccc1 10.1021/acs.jmedchem.4c00359
168279661 374155 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5187543 374155 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 420 5 2 5 4.0 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
178306932 467052 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 399 6 1 5 5.1 Oc1cc(COc2ccc(Cl)c3ccccc23)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6167439 467052 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 399 6 1 5 5.1 Oc1cc(COc2ccc(Cl)c3ccccc23)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
169561615 389856 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 446 10 1 5 6.9 CC/C=C\CCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5500184 389856 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 446 10 1 5 6.9 CC/C=C\CCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
178323803 467418 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 329 7 1 5 3.5 Oc1cc(COCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
CHEMBL6175761 467418 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 329 7 1 5 3.5 Oc1cc(COCc2ccccc2)nc(OCC2CCCCO2)c1 10.1021/acs.jmedchem.4c02335
178320777 467266 0 None -34 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
CHEMBL6172370 467266 0 None -34 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 343 7 1 5 4.0 CC(OCc1cc(O)cc(OCC2CCCCO2)n1)c1ccccc1 10.1021/acs.jmedchem.4c02335
168282833 374280 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 6 1 6 4.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5189536 374280 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 462 6 1 6 4.5 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccc(CN3CCOCC3)cc2)cc1 10.1021/acs.jmedchem.2c00804
24894958 390039 34 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 612 2 1 3 11.5 CC(C)(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(C)(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5512456 390039 34 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 612 2 1 3 11.5 CC(C)(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(C(C)(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
10171 3702 28 None 125 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
71616860 3702 28 None 125 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
CHEMBL3716365 3702 28 None 125 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
DB15346 3702 28 None 125 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
169561609 389664 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 447 11 2 4 6.7 CCCCCCCCNP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498727 389664 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 447 11 2 4 6.7 CCCCCCCCNP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
168271681 373442 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 490 8 3 5 4.1 CC(=O)NCCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5176916 373442 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 490 8 3 5 4.1 CC(=O)NCCNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
71617205 270441 2 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3719092 270441 2 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 3 0 6 2.0 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2 10.1021/acs.jmedchem.0c00272
89645365 271425 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715918 271425 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
153309830 385331 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1ccc2c(c1)C=C(OP(=O)(O)OC1=Cc3cc(OC)ccc3Sc3c(OC)cccc31)c1cccc(OC)c1S2 10.1021/acs.jmedchem.1c01813
CHEMBL5221361 385331 0 None None None Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 634 8 1 9 8.5 COc1ccc2c(c1)C=C(OP(=O)(O)OC1=Cc3cc(OC)ccc3Sc3c(OC)cccc31)c1cccc(OC)c1S2 10.1021/acs.jmedchem.1c01813
177638553 390141 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 947 13 2 10 12.4 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5517838 390141 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 947 13 2 10 12.4 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccccc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
146807714 385310 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 508 4 1 5 7.7 CN1c2ccccc2C=C(OP(=O)(O)OC2=Cc3ccccc3N(C)c3ccccc32)c2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221218 385310 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 508 4 1 5 7.7 CN1c2ccccc2C=C(OP(=O)(O)OC2=Cc3ccccc3N(C)c3ccccc32)c2ccccc21 10.1021/acs.jmedchem.1c01813
169561600 389707 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 460 4 1 4 7.1 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2c(F)cccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498999 389707 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 460 4 1 4 7.1 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2c(F)cccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
10708352 373088 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 286 3 1 3 3.6 c1ccc(-c2cnc(Cc3c[nH]c4ccccc34)nn2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5171020 373088 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 286 3 1 3 3.6 c1ccc(-c2cnc(Cc3c[nH]c4ccccc34)nn2)cc1 10.1021/acs.jmedchem.2c00804
101543344 390644 1 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 512 2 1 5 9.0 O=P1(O)Oc2c(-c3ccsc3)cc3ccccc3c2-c2c(c(-c3ccsc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5555830 390644 1 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 512 2 1 5 9.0 O=P1(O)Oc2c(-c3ccsc3)cc3ccccc3c2-c2c(c(-c3ccsc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
10171 3702 28 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
71616860 3702 28 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
CHEMBL3716365 3702 28 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
DB15346 3702 28 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP productionAntagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.1c01813
149484987 390125 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 586 4 1 5 9.0 CN(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(N(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517642 390125 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 586 4 1 5 9.0 CN(C)c1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(N(C)C)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
11211 8982 40 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
1912564 8982 40 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
CHEMBL3827756 8982 40 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.4c02335
156499983 467481 0 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6176923 467481 0 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 335 11 1 4 5.0 CCCCCCCCCc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
162656165 354740 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 353 4 0 6 2.6 COc1ccc2c(c1)CCn1c-2cc(OCc2ncccc2F)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL4757413 354740 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 353 4 0 6 2.6 COc1ccc2c(c1)CCn1c-2cc(OCc2ncccc2F)nc1=O 10.1021/acs.jmedchem.0c00272
89645206 271583 0 None 50 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassayAntagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3716446 271583 0 None 50 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassayAntagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in capric acid-induced IP1 accumulation treated for 30 mins prior to capric acid stimulation measured after 1 hr by HTRF based immunoassay
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
153309801 385465 0 None None None Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222213 385465 0 None None None Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 574 6 1 7 8.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
168285471 385460 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 458 8 1 3 7.5 O=P(O)(O/C(=C\c1ccccc1)C1C=CC=CC1)O/C(=C\c1ccccc1)C1C=CC=CC1 10.1021/acs.jmedchem.1c01813
CHEMBL5222190 385460 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 458 8 1 3 7.5 O=P(O)(O/C(=C\c1ccccc1)C1C=CC=CC1)O/C(=C\c1ccccc1)C1C=CC=CC1 10.1021/acs.jmedchem.1c01813
76684664 271505 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 342 4 0 6 2.4 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL3716185 271505 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 342 4 0 6 2.4 COc1ccc2c(c1)CCn1c-2cc(OCC2CCCCO2)nc1=O 10.1021/acs.jmedchem.0c00272
169561627 389765 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1ccc2ccccc2c1 10.1021/acs.jmedchem.3c00053
CHEMBL5499525 389765 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 462 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1ccc2ccccc2c1 10.1021/acs.jmedchem.3c00053
153309764 385441 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 506 4 1 5 6.6 O=c1c2ccccc2cc(OP(=O)(O)Oc2cc3ccccc3c(=O)c3ccccc23)c2ccccc12 10.1021/acs.jmedchem.1c01813
CHEMBL5222064 385441 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 506 4 1 5 6.6 O=c1c2ccccc2cc(OP(=O)(O)Oc2cc3ccccc3c(=O)c3ccccc23)c2ccccc12 10.1021/acs.jmedchem.1c01813
168281902 374166 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccnnc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5187711 374166 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 365 4 1 6 3.5 c1ccc(-c2nc(Cc3c[nH]c4cnccc34)nnc2-c2ccnnc2)cc1 10.1021/acs.jmedchem.2c00804
172203807 389720 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H]2CC[C@@]1(C)C2(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5499108 389720 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H]2CC[C@@]1(C)C2(C)C 10.1021/acs.jmedchem.3c00053
162655454 354644 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 394 7 0 7 2.9 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4756307 354644 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 394 7 0 7 2.9 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
168274043 373350 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 6 1 4 5.3 CN(C)Cc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5175411 373350 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 6 1 4 5.3 CN(C)Cc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561505 389698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCCC1 10.1021/acs.jmedchem.3c00053
CHEMBL5498945 389698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 432 5 1 5 6.5 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1CCCCCC1 10.1021/acs.jmedchem.3c00053
162642975 355500 0 None -67 2 Mouse 6.2 pIC50 = 6.2 Functional
Inverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassayInverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassay
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4776061 355500 0 None -67 2 Mouse 6.2 pIC50 = 6.2 Functional
Inverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassayInverse agonist activity at recombinant mouse GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction in IP1 accumulation incubated for 30 mins by HTRF based immunoassay
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
177374259 390495 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5542801 390495 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
23110764 390258 0 None None None Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 432 4 1 3 7.4 CCCc1cc2ccccc2c2c1OP(=O)(O)Oc1c(CCC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
CHEMBL5523382 390258 0 None None None Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 432 4 1 3 7.4 CCCc1cc2ccccc2c2c1OP(=O)(O)Oc1c(CCC)cc3ccccc3c1-2 10.1021/acs.jmedchem.4c00359
168281794 374034 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 475 5 1 5 4.8 O=C(c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1)N1CCOCC1 10.1021/acs.jmedchem.2c00804
CHEMBL5185972 374034 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 475 5 1 5 4.8 O=C(c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1)N1CCOCC1 10.1021/acs.jmedchem.2c00804
153309774 385491 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1ccc2c(c1)C(OP(=O)(O)OC1=Cc3ccccc3Sc3ccc(C)cc31)=Cc1ccccc1S2 10.1021/acs.jmedchem.1c01813
CHEMBL5222394 385491 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1ccc2c(c1)C(OP(=O)(O)OC1=Cc3ccccc3Sc3ccc(C)cc31)=Cc1ccccc1S2 10.1021/acs.jmedchem.1c01813
169561614 389701 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 468 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc(C)ccc1C(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5498953 389701 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 468 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)Oc1cc(C)ccc1C(C)C 10.1021/acs.jmedchem.3c00053
168292266 374924 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5199559 374924 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156500000 467164 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 405 8 1 5 4.7 CCCc1ccc(CCc2cc(O)cc(OCC3COc4ccccc4O3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6170239 467164 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 405 8 1 5 4.7 CCCc1ccc(CCc2cc(O)cc(OCC3COc4ccccc4O3)n2)cc1 10.1021/acs.jmedchem.4c02335
168287166 374687 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 5 1 5 4.7 CS(=O)(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5195677 374687 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 5 1 5 4.7 CS(=O)(=O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561651 389644 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C[C@H](C)CC[C@H]1C(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5498567 389644 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@@H]1C[C@H](C)CC[C@H]1C(C)C 10.1021/acs.jmedchem.3c00053
71616529 271347 0 None -36 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None -36 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at mouse Galphai2-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in PSB-16671-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
169561643 389643 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C(C)(C)[C@H]2CC[C@]1(C)C2 10.1021/acs.jmedchem.3c00053
CHEMBL5498557 389643 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 472 5 1 5 7.0 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C(C)(C)[C@H]2CC[C@]1(C)C2 10.1021/acs.jmedchem.3c00053
168271441 373689 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 392 5 2 4 4.8 OCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5180745 373689 0 None None None Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 392 5 2 4 4.8 OCc1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
69823296 390516 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2ccc3cc(-c4ccccc4)ccc3c2-c2c(ccc3cc(-c4ccccc4)ccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5543044 390516 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2ccc3cc(-c4ccccc4)ccc3c2-c2c(ccc3cc(-c4ccccc4)ccc23)O1 10.1021/acs.jmedchem.4c00359
71616529 271347 0 None 36 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715656 271347 0 None 36 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopyAntagonist activity at human Flag-tagged Gialpha-coupled GPR84 expressed in human Flp-In-T-REx-293 cell membrane assessed as reduction in ZQ-16-induced stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by ZQ-16 addition and subsequent addition of [35S]GTPgammaS measured after 60 mins by liquid scintillation spectroscopy
ChEMBL 443 5 1 7 2.7 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CCNc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
168269632 373122 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5171669 373122 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 362 4 1 3 5.3 c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
178317703 466849 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 285 5 1 4 3.1 CCCc1cc(O)cc(OCC2Cc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6162518 466849 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 285 5 1 4 3.1 CCCc1cc(O)cc(OCC2Cc3ccccc3O2)n1 10.1021/acs.jmedchem.4c02335
178306071 467157 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 8 1 6 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1OC 10.1021/acs.jmedchem.4c02335
CHEMBL6170011 467157 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 373 8 1 6 3.5 COc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1OC 10.1021/acs.jmedchem.4c02335
169561593 389713 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 426 4 1 4 6.6 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Oc2ccccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5499059 389713 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 426 4 1 4 6.6 CC1(C)[C@@H]2CC[C@@](C)(C2)[C@@H]1OP(=O)(O)OC1=Cc2ccccc2Oc2ccccc21 10.1021/acs.jmedchem.3c00053
71598639 272433 31 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.1c01813
CHEMBL3719364 272433 31 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 421 6 0 8 2.2 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(OCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.1c01813
23628846 389939 33 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 652 4 1 3 12.2 O=P1(O)Oc2c(-c3ccc(-c4ccccc4)cc3)cc3ccccc3c2-c2c(c(-c3ccc(-c4ccccc4)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5505750 389939 33 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 652 4 1 3 12.2 O=P1(O)Oc2c(-c3ccc(-c4ccccc4)cc3)cc3ccccc3c2-c2c(c(-c3ccc(-c4ccccc4)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
1758434 139328 7 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 363 5 1 6 3.1 COc1cc2c(cc1OC)-c1cc(NCc3ccccc3)nc(=O)n1CC2 10.1016/j.ejmech.2023.115762
CHEMBL1871173 139328 7 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 363 5 1 6 3.1 COc1cc2c(cc1OC)-c1cc(NCc3ccccc3)nc(=O)n1CC2 10.1016/j.ejmech.2023.115762
1758434 139328 7 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 363 5 1 6 3.1 COc1cc2c(cc1OC)-c1cc(NCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL1871173 139328 7 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 363 5 1 6 3.1 COc1cc2c(cc1OC)-c1cc(NCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
149469204 375057 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5201755 375057 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.3c00053
149469204 375057 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5201755 375057 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 514 4 1 5 8.4 O=P(O)(OC1=Cc2ccccc2Sc2ccccc21)OC1=Cc2ccccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
168292093 374980 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 303 6 0 3 4.9 CCCCCc1nnc(-c2ccccc2)c(-c2ccccc2)n1 10.1021/acs.jmedchem.2c00804
CHEMBL5200441 374980 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 303 6 0 3 4.9 CCCCCc1nnc(-c2ccccc2)c(-c2ccccc2)n1 10.1021/acs.jmedchem.2c00804
16050033 390144 34 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3cccc4ccccc34)cc3ccccc3c2-c2c(c(-c3cccc4ccccc34)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5517888 390144 34 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 600 2 1 3 11.2 O=P1(O)Oc2c(-c3cccc4ccccc34)cc3ccccc3c2-c2c(c(-c3cccc4ccccc34)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
146294463 390465 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 532 2 3 5 8.3 O=P1(O)Oc2c(-c3ccc(O)cc3)cc3ccccc3c2-c2c(c(-c3ccc(O)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5542432 390465 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 532 2 3 5 8.3 O=P1(O)Oc2c(-c3ccc(O)cc3)cc3ccccc3c2-c2c(c(-c3ccc(O)cc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
156499851 467333 0 None -37 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174163 467333 0 None -37 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assayAntagonist activity at mouse GPR84 expressed in Flp-In-T-REx-293 cells co-expressing Galphai2 assessed as IBMX/forskolin-induced cAMP accumulation pretreated with compound for 10 mins followed by IBMX/forskolin induction and measured after 15 mins by FRET assay
ChEMBL 355 8 1 4 4.5 CCCc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
89645206 271583 0 None 50 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3716446 271583 0 None 50 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 419 6 0 7 2.4 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(CCc3ccccn3)ccc1-2 10.1021/acs.jmedchem.0c00272
162642975 355500 0 None 67 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4776061 355500 0 None 67 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 395 7 0 8 2.3 COc1cc2c(cc1OC)-c1cc(OCCOc3ccccn3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
168297026 375431 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5207823 375431 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.7 c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
167175655 373170 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 434 6 1 5 5.3 CC(=O)OCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5172567 373170 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 434 6 1 5 5.3 CC(=O)OCc1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
153309768 385373 0 None 11 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221639 385373 0 None 11 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2c(Cl)cccc2Sc2ccccc21)OC1=Cc2c(Cl)cccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
162653421 354348 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 6 0 6 3.1 COc1cc2c(cc1OC)-c1cc(OCCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4752941 354348 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 378 6 0 6 3.1 COc1cc2c(cc1OC)-c1cc(OCCc3ccccc3)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
169561500 389676 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 434 10 1 5 6.8 CCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
CHEMBL5498805 389676 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 434 10 1 5 6.8 CCCCCCCOP(=O)(O)OC1=Cc2ccccc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.3c00053
89645365 271425 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3715918 271425 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of embelin-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 442 7 0 8 2.2 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1cc(COCC3CCOCC3)ccc1-2 10.1021/acs.jmedchem.0c01378
178317578 466742 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 377 7 1 5 4.3 Cc1cc(OCCc2cc(O)cc(OCC3CCCCO3)n2)ccc1Cl 10.1021/acs.jmedchem.4c02335
CHEMBL6159863 466742 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 377 7 1 5 4.3 Cc1cc(OCCc2cc(O)cc(OCC3CCCCO3)n2)ccc1Cl 10.1021/acs.jmedchem.4c02335
71616288 272027 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 409 6 1 8 2.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(NCc3ccco3)ccc1-2 10.1021/acs.jmedchem.0c00272
CHEMBL3718005 272027 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 409 6 1 8 2.5 O=c1nc(OCC2COCCO2)cc2n1CCc1cc(NCc3ccco3)ccc1-2 10.1021/acs.jmedchem.0c00272
162666623 356071 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 352 4 0 5 3.2 COc1ccc2c(c1)-c1cc(OCc3ccccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
CHEMBL4783553 356071 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 352 4 0 5 3.2 COc1ccc2c(c1)-c1cc(OCc3ccccc3F)nc(=O)n1CC2 10.1021/acs.jmedchem.0c00272
146294472 390730 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 502 2 1 5 7.7 O=P1(O)Oc2c(-c3cccnc3)cc3ccccc3c2-c2c(c(-c3cccnc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5557021 390730 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 502 2 1 5 7.7 O=P1(O)Oc2c(-c3cccnc3)cc3ccccc3c2-c2c(c(-c3cccnc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
71616526 271952 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL3717743 271952 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometryAntagonist activity at recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cells assessed as inhibition of DIM-induced [35S]GTPgammaS binding pre-incubated for 15 mins followed by [35S]GTPgammaS addition and measured after 45 mins by liquid scintillation spectrometry
ChEMBL 452 7 0 10 2.1 O=c1nc(OC[C@H]2COCCO2)cc2n1CCc1cc(OCc3noc(C4CC4)n3)ccc1-2 10.1021/acs.jmedchem.0c01378
168282493 373853 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5183310 373853 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 406 5 2 4 5.0 O=C(O)c1ccc(-c2nnc(Cc3c[nH]c4ccccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
168295842 375282 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 5 1 5 4.7 CS(=O)(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5205328 375282 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 440 5 1 5 4.7 CS(=O)(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
162650087 353987 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 393 4 0 8 2.1 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3cccnc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
CHEMBL4748375 353987 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting methodAntagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
ChEMBL 393 4 0 8 2.1 COc1ccc2c(c1)CCn1c-2cc(OCC2COc3cccnc3O2)nc1=O 10.1021/acs.jmedchem.0c00272
12151052 101596 42 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2c(-c3ccccc3)cc3ccccc3c2-c2c(c(-c3ccccc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL1554297 101596 42 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium responseAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU-induced calcium response
ChEMBL 500 2 1 3 8.9 O=P1(O)Oc2c(-c3ccccc3)cc3ccccc3c2-c2c(c(-c3ccccc3)cc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
153309757 385443 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2cc(Cl)ccc2Sc2ccccc21)OC1=Cc2cc(Cl)ccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5222073 385443 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 582 4 1 5 9.8 O=P(O)(OC1=Cc2cc(Cl)ccc2Sc2ccccc21)OC1=Cc2cc(Cl)ccc2Sc2ccccc21 10.1021/acs.jmedchem.1c01813
153309820 385364 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(C)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221528 385364 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 542 4 1 5 9.1 Cc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)OC1=Cc2ccccc2Sc2c(C)cccc21 10.1021/acs.jmedchem.1c01813
148925847 385367 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1cc(F)ccc1C=C2OP(=O)(O)OC1=Cc2ccc(F)cc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
CHEMBL5221558 385367 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium response preincubated for 10 mins followed by agonist addition and measured after 1 min by calcium mobilization assay
ChEMBL 610 6 1 7 8.7 COc1cccc2c1Sc1cc(F)ccc1C=C2OP(=O)(O)OC1=Cc2ccc(F)cc2Sc2c(OC)cccc21 10.1021/acs.jmedchem.1c01813
168271098 373165 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5172502 373165 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 419 5 2 4 4.6 CNC(=O)c1ccc(-c2nc(Cc3c[nH]c4ccccc34)nnc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
169561652 389711 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H](C)CC[C@@H]1C(C)C 10.1021/acs.jmedchem.3c00053
CHEMBL5499036 389711 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assayAntagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
ChEMBL 474 6 1 5 7.3 COc1cccc2c1Sc1ccccc1C=C2OP(=O)(O)O[C@H]1C[C@@H](C)CC[C@@H]1C(C)C 10.1021/acs.jmedchem.3c00053
178309761 467408 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 327 6 1 4 3.8 Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6175479 467408 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 327 6 1 4 3.8 Cc1ccc(CCc2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
168287306 374849 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 450 7 3 6 3.4 O=C(NCCO)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5198225 374849 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 450 7 3 6 3.4 O=C(NCCO)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156499991 466919 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 337 11 1 5 3.9 CCCCCCCCCc1cc(O)cc(OCC2COCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6164193 466919 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 337 11 1 5 3.9 CCCCCCCCCc1cc(O)cc(OCC2COCCO2)n1 10.1021/acs.jmedchem.4c02335
168297809 375285 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 4.5 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
CHEMBL5205398 375285 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysisAntagonist activity at human Galphai2-fused GPR84 stably expressed in Flp-In-T-REx-293 cell membranes assessed as inhibition of PSB-16671-induced [35S]GTPgammaS binding preincubated for 15 mins followed by PSB-16671 addition and measured after 45 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 4.5 COC(=O)c1ccc(-c2nnc(Cc3c[nH]c4cnccc34)nc2-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00804
156499996 467029 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 336 11 2 5 4.5 CCCCCCCCNc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
CHEMBL6166866 467029 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 336 11 2 5 4.5 CCCCCCCCNc1cc(O)cc(OCC2CCCCO2)n1 10.1021/acs.jmedchem.4c02335
156499952 467346 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 370 8 1 5 4.3 CCCc1ccc(CN(C)c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
CHEMBL6174338 467346 0 None None None Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assayAntagonist activity at human GPR84 expressed in HTLA cells co-expressing GPR84-tango plasmid assessed as beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by ZQ-16 addition and measured after 36 to 40 hrs by PRESTO-Tango assay
ChEMBL 370 8 1 5 4.3 CCCc1ccc(CN(C)c2cc(O)cc(OCC3CCCCO3)n2)cc1 10.1021/acs.jmedchem.4c02335
3893 4658 74 None -2 3 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
4642 4658 74 None -2 3 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
5534 4658 74 None -2 3 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
CHEMBL108766 4658 74 None -2 3 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
DB03017 4658 74 None -2 3 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
13103 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 38146625
171037436 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 38146625
CHEMBL5395893 6058 0 None None None Human 10.7 pEC50 = 10.7 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 331 4 1 2 3.9 ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F 38146625
11213 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 32869860
11213 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 38146625
154578239 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 32869860
154578239 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 38146625
CHEMBL4743442 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 32869860
CHEMBL4743442 2971 9 None None None Human 7.9 pEC50 = 7.9 Functional
Measured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cellsMeasured as inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells
Guide to Pharmacology 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 38146625
10717 6527 6 None None None Human 8.5 pEC50 = 8.5 Functional
Potency in a β-arrestin recruitment assay.Potency in a β-arrestin recruitment assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
44349321 6527 6 None None None Human 8.5 pEC50 = 8.5 Functional
Potency in a β-arrestin recruitment assay.Potency in a β-arrestin recruitment assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
CHEMBL124977 6527 6 None None None Human 8.5 pEC50 = 8.5 Functional
Potency in a β-arrestin recruitment assay.Potency in a β-arrestin recruitment assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
10717 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Potency in a cAMP assay.Potency in a cAMP assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
44349321 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Potency in a cAMP assay.Potency in a cAMP assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
CHEMBL124977 6527 6 None None None Human 8.3 pEC50 = 8.3 Functional
Potency in a cAMP assay.Potency in a cAMP assay.
Guide to Pharmacology 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 30023867
26612 205 63 None None None Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 23449982
5848 205 63 None None None Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 23449982
CHEMBL4448230 205 63 None None None Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 23449982
21488 136 0 None None None Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 8 2 2 2.2 CCCCCCCCC(C(=O)O)O 23449982
5847 136 0 None None None Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 8 2 2 2.2 CCCCCCCCC(C(=O)O)O 23449982
5850 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 23449982
94216 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 23449982
CHEMBL4288936 207 53 None None None Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 23449982
5849 138 40 None -1 2 Human 5.0 pEC50 = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 23449982
97783 138 40 None -1 2 Human 5.0 pEC50 = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 23449982
CHEMBL4278254 138 40 None -1 2 Human 5.0 pEC50 = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 23449982
3893 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 16966319
4642 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 16966319
5534 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 16966319
CHEMBL108766 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 16966319
DB03017 4658 74 None -2 3 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 16966319
5533 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 16966319
8180 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 16966319
CHEMBL108030 8561 70 None None None Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 16966319
2969 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 16966319
2969 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 23396314
5532 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 16966319
5532 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 23396314
CHEMBL107498 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 16966319
CHEMBL107498 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 23396314
DB03600 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 16966319
DB03600 2799 70 None None None Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 172 8 1 1 3.2 CCCCCCCCCC(=O)O 23396314
10354234 335 45 None None None Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 23449982
125356668 335 45 None None None Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 23449982
5846 335 45 None None None Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 23449982
CHEMBL3827832 335 45 None None None Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 23449982
133081959 6533 4 None None None Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 30023867
9871 6533 4 None None None Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 30023867
CHEMBL4444010 6533 4 None None None Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 30023867
12819 6131 0 None None None Human 4.8 pIC50 = 4.8 Functional
Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.
Guide to Pharmacology 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 32728158
140700741 6131 0 None None None Human 4.8 pIC50 = 4.8 Functional
Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.
Guide to Pharmacology 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 32728158
78319081 6131 0 None None None Human 4.8 pIC50 = 4.8 Functional
Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.
Guide to Pharmacology 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 32728158
CHEMBL4803197 6131 0 None None None Human 4.8 pIC50 = 4.8 Functional
Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.Antagonisn of sodium decanoate-mediated GPR84 activation, determined in a BRET biosensor assay measuring Gαi protein activation in HEK293 cells.
Guide to Pharmacology 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 32728158
14448 3763 0 None None None Human 6.6 pIC50 = 6.6 Functional
Determined in a [<sup>35</sup>S]GTP&gamma;S incorporation (functional) assay, in Flp-ln TREx HEK293 cells stably expressing hGPR84 treated with agonist ZQ-16 (2-HTP)Determined in a [<sup>35</sup>S]GTP&gamma;S incorporation (functional) assay, in Flp-ln TREx HEK293 cells stably expressing hGPR84 treated with agonist ZQ-16 (2-HTP)
Guide to Pharmacology 356 3 1 3 2.9 CC(=O)N1C[C@H]([C@H]2COC3=C(C=CC=C3)[C@@H]12)C(=O)NCC4CCCCC4 41870364
10043 7306 0 None None None Human 3.4 pIC50 = 3.4 Functional
Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
24749700 7306 0 None None None Human 3.4 pIC50 = 3.4 Functional
Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
DB15447 7306 0 None None None Human 3.4 pIC50 = 3.4 Functional
Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.Measuring antagonist-dependent inhibition of G&alpha;<sub>i</sub>activation by sodium decanoate (agonist) in receptor transfected HEK293 cells.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
13892 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 40183744
156499897 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 40183744
CHEMBL6161601 8446 3 None 43 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 8 1 5 3.9 CCOC1=CC=C(CCC2=NC(OCC3CCCCO3)=CC(O)=C2)C=C1 40183744


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
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2969 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
5532 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL107498 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
DB03600 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
2969 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 5.0 pEC50 = 5 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
9944370 193930 3 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL246298 193930 3 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.9b01339
137649817 313311 0 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.6b01593
CHEMBL4078546 313311 0 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.6b01593
133081959 6533 4 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
9871 6533 4 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4444010 6533 4 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
137649231 313045 0 None None None Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4075099 313045 0 None None None Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
10354234 335 45 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
125356668 335 45 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
5846 335 45 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827832 335 45 None None None Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.0c01378
10354234 335 45 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
9944370 193930 3 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL246298 193930 3 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 306 4 2 2 4.3 COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/acs.jmedchem.6b01593
137658671 315290 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4101219 315290 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
11209 3191 70 None None None Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
3218 3191 70 None None None Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL221137 3191 70 None None None Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
137658184 315583 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.9b01339
CHEMBL4104992 315583 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.9b01339
137658671 315290 0 None None None Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.9b01339
CHEMBL4101219 315290 0 None None None Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.9b01339
11208 2931 74 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
3071 2931 74 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
CHEMBL446452 2931 74 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
DB11875 2931 74 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01593
12530 20123 64 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107874 20123 64 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB02448 20123 64 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
137632827 312315 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 10.1021/acs.jmedchem.9b01339
CHEMBL4066454 312315 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 10.1021/acs.jmedchem.9b01339
10354234 335 45 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
12380289 314071 2 None None None Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4087824 314071 2 None None None Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
12380289 314071 2 None None None Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
CHEMBL4087824 314071 2 None None None Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 260 2 2 1 3.9 O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
9882204 315330 21 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4101728 315330 21 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.9b01339
12037446 315605 0 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 248 2 2 2 3.0 c1cnc2[nH]cc(Cc3c[nH]c4ncccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4105236 315605 0 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 248 2 2 2 3.0 c1cnc2[nH]cc(Cc3c[nH]c4ncccc34)c2c1 10.1021/acs.jmedchem.6b01593
9901435 314854 2 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1ccc2[nH]cc(Cc3c[nH]c4ccc(Cl)cc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4096406 314854 2 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1ccc2[nH]cc(Cc3c[nH]c4ccc(Cl)cc34)c2c1 10.1021/acs.jmedchem.9b01339
137649231 313045 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4075099 313045 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 264 2 2 0 4.4 Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.9b01339
11150029 313891 5 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 274 3 2 0 5.2 CCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4085470 313891 5 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 274 3 2 0 5.2 CCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
2778732 314021 60 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 153 0 1 0 2.4 Fc1cc2cc[nH]c2cc1F 10.1021/acs.jmedchem.6b01593
CHEMBL4087204 314021 60 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 153 0 1 0 2.4 Fc1cc2cc[nH]c2cc1F 10.1021/acs.jmedchem.6b01593
10717 6527 6 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
44349321 6527 6 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL124977 6527 6 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
72711216 313652 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4082668 313652 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.9b01339
5850 207 53 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
94216 207 53 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4288936 207 53 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
3893 4658 74 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
4642 4658 74 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5534 4658 74 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108766 4658 74 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03017 4658 74 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
11208 2931 74 None None None Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
3071 2931 74 None None None Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
CHEMBL446452 2931 74 None None None Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
DB11875 2931 74 None None None Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 246 2 2 0 4.2 c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 10.1021/acs.jmedchem.9b01339
137658184 315583 0 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.6b01593
CHEMBL4104992 315583 0 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 350 2 2 0 5.8 Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl 10.1021/acs.jmedchem.6b01593
11209 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
3218 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL221137 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
26612 205 63 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
5848 205 63 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4448230 205 63 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
137643701 314156 2 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4088884 314156 2 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.9b01339
11209 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
3218 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL221137 3191 70 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human PK-tagged GPR84 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase complementation assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.6b01593
16064 327827 56 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4456892 327827 56 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
9882204 315330 21 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4101728 315330 21 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
5533 8561 70 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
8180 8561 70 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108030 8561 70 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
1563 145124 51 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL2004471 145124 51 None None None Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
5288266 40330 44 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL1232858 40330 44 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
DB02767 40330 44 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
102583156 314776 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4095532 314776 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.9b01339
11212 337 2 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assayAgonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
127045422 337 2 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assayAgonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3828298 337 2 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assayAgonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
11209 3191 70 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
11212 337 2 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
127045422 337 2 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3828298 337 2 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
137649817 313311 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.9b01339
CHEMBL4078546 313311 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F 10.1021/acs.jmedchem.9b01339
11210 6531 3 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025748 6531 3 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4538049 6531 3 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
102219035 315231 0 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 314 2 2 0 5.5 Clc1ccc2c(Cc3c[nH]c4cc(Cl)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4100658 315231 0 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 314 2 2 0 5.5 Clc1ccc2c(Cc3c[nH]c4cc(Cl)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
137643701 314156 2 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4088884 314156 2 None None None Human 5.3 pEC50 = 5.3 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 318 2 2 0 4.8 Fc1cc(F)c2[nH]cc(Cc3c[nH]c4c(F)cc(F)cc34)c2c1 10.1021/acs.jmedchem.6b01593
10201214 193994 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 402 2 2 0 5.8 Brc1ccc2[nH]cc(Cc3c[nH]c4ccc(Br)cc34)c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL246504 193994 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 402 2 2 0 5.8 Brc1ccc2[nH]cc(Cc3c[nH]c4ccc(Br)cc34)c2c1 10.1021/acs.jmedchem.9b01339
11211 8982 40 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
137635702 311972 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.6b01593
CHEMBL4062512 311972 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.6b01593
10266133 312092 10 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4063898 312092 10 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
2969 2799 70 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
5532 2799 70 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
CHEMBL107498 2799 70 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
DB03600 2799 70 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b01593
137635702 311972 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.9b01339
CHEMBL4062512 311972 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 282 2 2 0 4.5 Fc1cccc2c(Cc3c[nH]c4c(F)cccc34)c[nH]c12 10.1021/acs.jmedchem.9b01339
102583156 314776 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4095532 314776 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 276 3 2 1 4.2 COc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 10.1021/acs.jmedchem.6b01593
11005 5494 74 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
2806 5494 74 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL111077 5494 74 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB08231 5494 74 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
11507535 315145 0 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4099626 315145 0 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
72711216 313652 0 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
CHEMBL4082668 313652 0 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
ChEMBL 282 2 2 0 4.5 Fc1ccc2c(Cc3c[nH]c4cc(F)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.6b01593
11211 8982 40 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
1912564 8982 40 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
CHEMBL3827756 8982 40 None None None Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.0c01378
137654126 314868 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)c(F)c34)c2c1F 10.1021/acs.jmedchem.9b01339
CHEMBL4096571 314868 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
ChEMBL 318 2 2 0 4.8 Fc1ccc2[nH]cc(Cc3c[nH]c4ccc(F)c(F)c34)c2c1F 10.1021/acs.jmedchem.9b01339
9878666 193929 2 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 2 0 2 4.3 Cn1cc(Cc2cn(C)c3ccccc23)c2ccccc21 10.1021/acs.jmedchem.9b01339
CHEMBL246297 193929 2 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 2 0 2 4.3 Cn1cc(Cc2cn(C)c3ccccc23)c2ccccc21 10.1021/acs.jmedchem.9b01339
12819 6131 0 None None None Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assayAntagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assay
ChEMBL 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 10.1021/acs.jmedchem.0c01378
140700741 6131 0 None None None Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assayAntagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assay
ChEMBL 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 10.1021/acs.jmedchem.0c01378
78319081 6131 0 None None None Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assayAntagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assay
ChEMBL 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 10.1021/acs.jmedchem.0c01378
CHEMBL4803197 6131 0 None None None Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assayAntagonist activity at human C-terminal GFP10-fused GPR84 expressed in HEK293 cells co-expressing Rluc8-tagged Galphai2/GFP10-tagged Ggamma2/Gbeta1 assessed as inhibition of embelin-induced Galphai activation incubated for 10 mins by BRET assay
ChEMBL 275 10 0 2 3.4 C(CCCC)C=1C=C(C=C(C1)CCCCC)CC(=O)[O-] 10.1021/acs.jmedchem.0c01378
10266133 312092 10 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
CHEMBL4063898 312092 10 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
102219035 315231 0 None None None Human 4.4 pIC50 = 4.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1ccc2c(Cc3c[nH]c4cc(Cl)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.9b01339
CHEMBL4100658 315231 0 None None None Human 4.4 pIC50 = 4.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 314 2 2 0 5.5 Clc1ccc2c(Cc3c[nH]c4cc(Cl)ccc34)c[nH]c2c1 10.1021/acs.jmedchem.9b01339
11150029 313891 5 None None None Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 3 2 0 5.2 CCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
CHEMBL4085470 313891 5 None None None Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 3 2 0 5.2 CCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.9b01339
162672882 366468 0 None None None Human 9.6 pKd = 9.6 Binding
Binding affinity to recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membrane incubated for 1 hr by liquid scintillation spectrometryBinding affinity to recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membrane incubated for 1 hr by liquid scintillation spectrometry
ChEMBL 440 8 0 7 3.5 O=c1nc(OCCOc2cnccn2)cc2n1CCc1cc(CCc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
CHEMBL4794652 366468 0 None None None Human 9.6 pKd = 9.6 Binding
Binding affinity to recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membrane incubated for 1 hr by liquid scintillation spectrometryBinding affinity to recombinant human N-terminal epitope tagged/eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membrane incubated for 1 hr by liquid scintillation spectrometry
ChEMBL 440 8 0 7 3.5 O=c1nc(OCCOc2cnccn2)cc2n1CCc1cc(CCc3ccccc3)ccc1-2 10.1021/acs.jmedchem.0c01378
177374259 390495 0 None None None Human 5.0 pKd = 5.0 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5542801 390495 0 None None None Human 5.0 pKd = 5.0 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
12151053 390157 36 None None None Human 6.0 pKd = 6.0 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517998 390157 36 None None None Human 6.0 pKd = 6.0 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
177374259 390495 0 None None None Human 6.8 pKd = 6.8 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
CHEMBL5542801 390495 0 None None None Human 6.8 pKd = 6.8 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 1448 46 2 22 12.2 CCN(CC)c1ccc2nc3c4cc(OCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc5ccc(-c6cc7ccccc7c7c6OP(=O)(O)Oc6c(-c8ccc(OC)cc8)cc8ccccc8c6-7)cc5)ccc4c(=O)cc-3oc2c1 10.1021/acs.jmedchem.4c00359
99589 390841 70 None None None Human 5.7 pKd = 5.7 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5558714 390841 70 None None None Human 5.7 pKd = 5.7 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
99589 390841 70 None None None Human 5.4 pKd = 5.4 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
CHEMBL5558714 390841 70 None None None Human 5.4 pKd = 5.4 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 348 0 1 3 5.5 O=P1(O)Oc2ccc3ccccc3c2-c2c(ccc3ccccc23)O1 10.1021/acs.jmedchem.4c00359
12151053 390157 36 None None None Human 7.2 pKd = 7.2 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
CHEMBL5517998 390157 36 None None None Human 7.2 pKd = 7.2 Binding
Binding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 minsBinding affinity at human GPR84 expressed in HEK293 cells assessed as dissociation constant measured upto 60 mins
ChEMBL 560 4 1 5 8.9 COc1ccc(-c2cc3ccccc3c3c2OP(=O)(O)Oc2c(-c4ccc(OC)cc4)cc4ccccc4c2-3)cc1 10.1021/acs.jmedchem.4c00359
11211 8982 40 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
1912564 8982 40 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827756 8982 40 None None None Human 9.7 pKi = 9.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
133081959 6533 4 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
9871 6533 4 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4444010 6533 4 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 309 4 3 3 1.5 Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
127045103 278368 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 276 6 2 5 3.0 Oc1cc(O)nc(SCCCCc2ccccc2)n1 10.1021/acs.jmedchem.9b01339
CHEMBL3827310 278368 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 276 6 2 5 3.0 Oc1cc(O)nc(SCCCCc2ccccc2)n1 10.1021/acs.jmedchem.9b01339
309844 473487 1 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 259 6 3 5 2.3 Oc1cc(NCCCCc2ccccc2)nc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL88536 473487 1 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 259 6 3 5 2.3 Oc1cc(NCCCCc2ccccc2)nc(O)n1 10.1021/acs.jmedchem.9b01339
146025749 348232 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 259 5 3 3 1.3 CCc1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
CHEMBL4547165 348232 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 259 5 3 3 1.3 CCc1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
10354234 335 45 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
125356668 335 45 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5846 335 45 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3827832 335 45 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 8 3 3 1.8 CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11210 6531 3 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025748 6531 3 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4538049 6531 3 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 Clc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
127045635 278452 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 262 5 2 5 2.6 Oc1cc(O)nc(SCCCc2ccccc2)n1 10.1021/acs.jmedchem.9b01339
CHEMBL3828415 278452 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 262 5 2 5 2.6 Oc1cc(O)nc(SCCCc2ccccc2)n1 10.1021/acs.jmedchem.9b01339
44349289 40909 1 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 267 10 3 5 3.4 CCCCCCCCCCNc1cc(O)nc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL125436 40909 1 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 267 10 3 5 3.4 CCCCCCCCCCNc1cc(O)nc(O)n1 10.1021/acs.jmedchem.9b01339
146025740 336378 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 7 3 3 1.4 CCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4468895 336378 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 7 3 3 1.4 CCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025741 347271 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 253 9 3 3 2.2 CCCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4521587 347271 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 253 9 3 3 2.2 CCCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025746 334389 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 245 4 3 3 1.0 Cc1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
CHEMBL4439640 334389 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 245 4 3 3 1.0 Cc1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
146025751 349628 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 287 4 3 3 2.0 CC(C)(C)c1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
CHEMBL4580884 349628 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 287 4 3 3 2.0 CC(C)(C)c1ccc(CCNc2cc(=O)[nH]c(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
11212 337 2 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
127045422 337 2 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL3828298 337 2 None None None Human 8.8 pKi = 8.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11212 337 2 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
127045422 337 2 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3828298 337 2 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 237 8 2 2 3.4 CCCCCCCCCc1cc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
308653 216553 5 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 231 4 3 5 1.5 Oc1cc(NCCc2ccccc2)nc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL314575 216553 5 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 231 4 3 5 1.5 Oc1cc(NCCc2ccccc2)nc(O)n1 10.1021/acs.jmedchem.9b01339
5796 140 57 None None None Human 4.0 pKi = 4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 10.1021/acs.jmedchem.9b01339
6995013 140 57 None None None Human 4.0 pKi = 4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 10.1021/acs.jmedchem.9b01339
94180 140 57 None None None Human 4.0 pKi = 4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4447980 140 57 None None None Human 4.0 pKi = 4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 10.1021/acs.jmedchem.9b01339
DB07907 140 57 None None None Human 4.0 pKi = 4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 10.1021/acs.jmedchem.9b01339
5533 8561 70 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
8180 8561 70 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108030 8561 70 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 186 9 1 1 3.6 CCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
146025747 348959 1 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2ccc(F)cc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4565153 348959 1 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2ccc(F)cc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5850 207 53 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
94216 207 53 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4288936 207 53 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 216 10 2 2 3.0 CCCCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
70521246 346928 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 240 6 2 4 0.8 CCCCCCOC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4513706 346928 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 240 6 2 4 0.8 CCCCCCOC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
171037982 391251 2 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
CHEMBL5565525 391251 2 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 257 5 2 2 2.8 CCCc1ccc(CCc2cc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.3c01923
171037986 391601 2 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5571529 391601 2 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 280 3 2 4 2.9 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)nc2)[nH]1 10.1021/acs.jmedchem.3c01923
155564247 349417 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 312 2 2 4 0.9 O=c1cc(N2CCN(C3CCc4ccccc43)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4575870 349417 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 312 2 2 4 0.9 O=c1cc(N2CCN(C3CCc4ccccc43)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
177648720 392169 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5591819 392169 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 279 3 2 3 3.5 O=c1cc(O)cc(-c2ccc(Oc3ccccc3)cc2)[nH]1 10.1021/acs.jmedchem.3c01923
136342308 334565 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 256 7 2 5 2.6 CCCCCCSc1nc(O)cc(C(=O)O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL4442407 334565 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 256 7 2 5 2.6 CCCCCCSc1nc(O)cc(C(=O)O)n1 10.1021/acs.jmedchem.9b01339
110698284 348508 1 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 5 3 3 -0.0 CCCCCNC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4554014 348508 1 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 5 3 3 -0.0 CCCCCNC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
110698276 335189 1 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 273 5 3 3 0.4 O=C(NCCCc1ccccc1)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4451263 335189 1 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 273 5 3 3 0.4 O=C(NCCCc1ccccc1)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11211 8982 40 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
1912564 8982 40 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL3827756 8982 40 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 228 6 2 4 2.1 CCCCCCSc1nc(O)cc(=O)[nH]1 10.1021/acs.jmedchem.3c01923
2969 2799 70 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5532 2799 70 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107498 2799 70 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03600 2799 70 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 172 8 1 1 3.2 CCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
146025759 347081 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 285 3 2 3 1.5 O=c1cc(N2CCC(Cc3ccccc3)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4517538 347081 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 285 3 2 3 1.5 O=c1cc(N2CCC(Cc3ccccc3)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025763 334083 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 6 3 5 1.5 O=Nc1c(NCCCc2ccccc2)[nH]c(=O)[nH]c1=O 10.1021/acs.jmedchem.9b01339
CHEMBL4434708 334083 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 274 6 3 5 1.5 O=Nc1c(NCCCc2ccccc2)[nH]c(=O)[nH]c1=O 10.1021/acs.jmedchem.9b01339
12530 20123 64 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL107874 20123 64 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB02448 20123 64 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 214 11 1 1 4.4 CCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
135372298 220022 68 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 144 6 1 1 2.4 CCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
379 220022 68 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 144 6 1 1 2.4 CCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
3998 220022 68 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 144 6 1 1 2.4 CCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL324846 220022 68 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 144 6 1 1 2.4 CCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB04519 220022 68 None None None Human 4.7 pKi = 4.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 144 6 1 1 2.4 CCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
309859 347533 1 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 261 6 3 4 0.9 O=c1cc(NCCCOc2ccccc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4528940 347533 1 None None None Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 261 6 3 4 0.9 O=c1cc(NCCCOc2ccccc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025758 349232 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 299 4 3 3 2.0 O=c1cc(NCCc2ccc(Cl)cc2Cl)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4571353 349232 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 299 4 3 3 2.0 O=c1cc(NCCc2ccc(Cl)cc2Cl)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
155513228 334314 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 282 4 2 4 2.5 O=c1cc(O)nc(SCCc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4438595 334314 0 None None None Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 282 4 2 4 2.5 O=c1cc(O)nc(SCCc2ccc(Cl)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
10717 6527 6 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
44349321 6527 6 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL124977 6527 6 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 211 6 3 3 1.1 CCCCCCNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
3893 4658 74 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
4642 4658 74 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
5534 4658 74 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL108766 4658 74 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB03017 4658 74 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
155525380 335556 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 289 6 3 3 1.8 CCCCCCNc1[nH]c(=O)[nH]c(=O)c1Br 10.1021/acs.jmedchem.9b01339
CHEMBL4456565 335556 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 289 6 3 3 1.8 CCCCCCNc1[nH]c(=O)[nH]c(=O)c1Br 10.1021/acs.jmedchem.9b01339
11209 3191 70 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
3218 3191 70 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL221137 3191 70 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 294 10 2 4 4.3 CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O 10.1021/acs.jmedchem.9b01339
11005 5494 74 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
2806 5494 74 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL111077 5494 74 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
DB08231 5494 74 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.9b01339
146025742 335474 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 241 8 4 4 0.4 O=c1cc(NCCCCCCCO)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4455292 335474 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 241 8 4 4 0.4 O=c1cc(NCCCCCCCO)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
308775 347516 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 247 5 3 4 0.6 O=c1cc(NCCOc2ccccc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4528577 347516 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 247 5 3 4 0.6 O=c1cc(NCCOc2ccccc2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
155559672 348868 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 326 4 2 4 2.6 O=c1cc(O)nc(SCCc2ccc(Br)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4562761 348868 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 326 4 2 4 2.6 O=c1cc(O)nc(SCCc2ccc(Br)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
155549030 347754 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 262 4 2 4 2.1 Cc1ccc(CCSc2nc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
CHEMBL4534827 347754 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 262 4 2 4 2.1 Cc1ccc(CCSc2nc(O)cc(=O)[nH]2)cc1 10.1021/acs.jmedchem.9b01339
146025745 349118 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 253 8 2 3 1.9 CCCCCCCCN(C)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4568775 349118 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 253 8 2 3 1.9 CCCCCCCCN(C)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
140898903 336301 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 266 4 2 4 1.9 O=c1cc(O)nc(SCCc2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4467630 336301 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 266 4 2 4 1.9 O=c1cc(O)nc(SCCc2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
146025754 336364 1 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 309 4 3 3 1.5 O=c1cc(NCCc2cccc(Br)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4468678 336364 1 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 309 4 3 3 1.5 O=c1cc(NCCc2cccc(Br)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
10171 3702 28 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
71616860 3702 28 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
CHEMBL3716365 3702 28 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
DB15346 3702 28 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 10.1021/acs.jmedchem.0c00272
1563 145124 51 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL2004471 145124 51 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCCC(O)C(=O)O 10.1021/acs.jmedchem.9b01339
26612 205 63 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
5848 205 63 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4448230 205 63 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 188 8 2 2 2.2 CCCCCCCC(CC(=O)O)O 10.1021/acs.jmedchem.9b01339
155560912 349000 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 317 8 3 3 2.6 CCCCCCCCNc1[nH]c(=O)[nH]c(=O)c1Br 10.1021/acs.jmedchem.9b01339
CHEMBL4566117 349000 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 317 8 3 3 2.6 CCCCCCCCNc1[nH]c(=O)[nH]c(=O)c1Br 10.1021/acs.jmedchem.9b01339
15549641 348639 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 212 6 1 4 2.9 CCCCCCSc1nccc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL4557017 348639 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 212 6 1 4 2.9 CCCCCCSc1nccc(O)n1 10.1021/acs.jmedchem.9b01339
146025755 335070 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2ccccc2F)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4449633 335070 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2ccccc2F)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025756 347726 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 O=c1cc(NCCc2ccccc2Cl)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4534071 347726 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 O=c1cc(NCCc2ccccc2Cl)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
155564383 349360 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 316 4 2 4 2.8 O=c1cc(O)nc(SCCc2ccc(C(F)(F)F)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4574495 349360 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 316 4 2 4 2.8 O=c1cc(O)nc(SCCc2ccc(C(F)(F)F)cc2)[nH]1 10.1021/acs.jmedchem.9b01339
135412234 334608 12 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 226 6 1 4 3.2 CCCCCCSc1nc(C)cc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL4442902 334608 12 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 226 6 1 4 3.2 CCCCCCSc1nc(C)cc(O)n1 10.1021/acs.jmedchem.9b01339
12782103 335936 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 268 9 3 5 2.2 CCCCCCCCNc1[nH]c(=O)[nH]c(=O)c1N=O 10.1021/acs.jmedchem.9b01339
CHEMBL4462370 335936 1 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 268 9 3 5 2.2 CCCCCCCCNc1[nH]c(=O)[nH]c(=O)c1N=O 10.1021/acs.jmedchem.9b01339
155551005 348014 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 209 5 3 3 0.8 CCC/C=C/CNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4541166 348014 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 209 5 3 3 0.8 CCC/C=C/CNc1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025753 336740 1 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 O=c1cc(NCCc2cccc(Cl)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4473999 336740 1 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 265 4 3 3 1.4 O=c1cc(NCCc2cccc(Cl)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
146025760 349765 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 306 2 2 4 1.0 O=c1cc(N2CCN(c3ccc(Cl)cc3)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4584001 349765 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 306 2 2 4 1.0 O=c1cc(N2CCN(c3ccc(Cl)cc3)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
21204487 347145 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 6 3 3 0.4 CCCCCCNC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4518826 347145 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 239 6 3 3 0.4 CCCCCCNC(=O)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
5288266 40330 44 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL1232858 40330 44 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
DB02767 40330 44 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCC[C@@H](O)CC(=O)O 10.1021/acs.jmedchem.9b01339
121205397 336231 8 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 237 4 3 4 0.8 O=c1cc(NCCc2cccs2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4466657 336231 8 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 237 4 3 4 0.8 O=c1cc(NCCc2cccs2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
86293760 336481 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 270 4 4 3 1.2 O=c1cc(NCCc2c[nH]c3ccccc23)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4470574 336481 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 270 4 4 3 1.2 O=c1cc(NCCc2c[nH]c3ccccc23)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
16064 327827 56 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
CHEMBL4456892 327827 56 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 244 12 2 2 3.7 CCCCCCCCCCCC(O)CC(=O)O 10.1021/acs.jmedchem.9b01339
146025762 349370 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 254 8 3 5 1.8 CCCCCCCNc1[nH]c(=O)[nH]c(=O)c1N=O 10.1021/acs.jmedchem.9b01339
CHEMBL4574715 349370 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 254 8 3 5 1.8 CCCCCCCNc1[nH]c(=O)[nH]c(=O)c1N=O 10.1021/acs.jmedchem.9b01339
177648470 392091 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
CHEMBL5590375 392091 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 263 6 2 2 3.8 O=c1cc(O)cc(CCCCCC2CCCCC2)[nH]1 10.1021/acs.jmedchem.3c01923
146025744 335250 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 6 2 3 1.1 CCCCCCN(C)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4451909 335250 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 225 6 2 3 1.1 CCCCCCN(C)c1cc(=O)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
155526533 335731 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 336 3 2 4 1.5 O=c1cc(N2CCN(Cc3cccc4ccccc34)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4459188 335731 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 336 3 2 4 1.5 O=c1cc(N2CCN(Cc3cccc4ccccc34)CC2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
11213 2971 9 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
154578239 2971 9 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
CHEMBL4743442 2971 9 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysisDisplacement of [3H]140 from GPR84 (unknown origin) expressed in Flp-In-T-REx-293 cells transfected with GalphaI incubated for 1 hr by liquid scintillation spectrometry analysis
ChEMBL 299 4 0 2 3.7 [O-][n+]1cccc(c1)CCOc1ccc(c2c1cccc2)Cl 10.1021/acs.jmedchem.3c01923
146025752 336781 1 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2cccc(F)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
CHEMBL4474487 336781 1 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 249 4 3 3 0.9 O=c1cc(NCCc2cccc(F)c2)[nH]c(=O)[nH]1 10.1021/acs.jmedchem.9b01339
309900 40599 1 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 197 5 3 5 1.5 CCCCCNc1cc(O)nc(O)n1 10.1021/acs.jmedchem.9b01339
CHEMBL124310 40599 1 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
ChEMBL 197 5 3 5 1.5 CCCCCNc1cc(O)nc(O)n1 10.1021/acs.jmedchem.9b01339
10171 3702 28 None None None Human 9.0 pIC50 = 9 Binding
Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.
Guide to Pharmacology 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 None
71616860 3702 28 None None None Human 9.0 pIC50 = 9 Binding
Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.
Guide to Pharmacology 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 None
CHEMBL3716365 3702 28 None None None Human 9.0 pIC50 = 9 Binding
Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.
Guide to Pharmacology 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 None
DB15346 3702 28 None None None Human 9.0 pIC50 = 9 Binding
Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.Binned data from [<sup>35</sup>S] GTP&gamma;S binding experiments using menbranes from cell that stably express GPR84.
Guide to Pharmacology 378 3 0 6 2.0 O=c1nc(OC[C@@H]2COCCO2)cc2n1CCc1c2ccc(c1)C#CC1CC1 None
135372298 220022 68 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
Drug Central 144 6 1 1 2.4 CCCCCCCC(=O)O None
379 220022 68 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
Drug Central 144 6 1 1 2.4 CCCCCCCC(=O)O None
3998 220022 68 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
Drug Central 144 6 1 1 2.4 CCCCCCCC(=O)O None
CHEMBL324846 220022 68 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
Drug Central 144 6 1 1 2.4 CCCCCCCC(=O)O None
DB04519 220022 68 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting methodDisplacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method
Drug Central 144 6 1 1 2.4 CCCCCCCC(=O)O None
14448 3763 0 None None None Human 8.2 pKi = 8.2 Binding
Determined in a competition binding study, dispalcing orthosteric antagonist [<sup>3</sup>H]140Determined in a competition binding study, dispalcing orthosteric antagonist [<sup>3</sup>H]140
Guide to Pharmacology 356 3 1 3 2.9 CC(=O)N1C[C@H]([C@H]2COC3=C(C=CC=C3)[C@@H]12)C(=O)NCC4CCCCC4 41870364