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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(-log)		 Activity
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1218 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
12668019 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
6603994 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL1160787 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL1317463 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 7350 28 None 67 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
86764103 260305 22 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 260305 22 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
11938 4900 10 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 4900 10 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 4900 10 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
681 3019 53 None 1 10 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 3019 53 None 1 10 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 3019 53 None 1 10 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 3019 53 None 1 10 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 3019 53 None 1 10 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
75202022 335355 7 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 335355 7 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
11681599 156841 0 None None None Human 10.3 pKi = 10.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 156841 0 None None None Human 10.3 pKi = 10.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
11623343 278114 0 None None None Human 9.3 pKi = 9.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 278114 0 None None None Human 9.3 pKi = 9.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11493746 278556 0 None None None Human 8.9 pKi = 8.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 278556 0 None None None Human 8.9 pKi = 8.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
11595240 277476 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 277476 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11558055 145361 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 145361 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 145361 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 145361 0 None None None Human 8.8 pKi = 8.8 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11522339 156920 0 None None None Human 8.0 pKi = 8.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 156920 0 None None None Human 8.0 pKi = 8.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
11500677 278120 0 None None None Human 6.0 pKi = 6.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 278120 0 None None None Human 6.0 pKi = 6.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
11573806 157083 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 157083 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
5249952 145616 5 None None None Human 7.0 pKi = 7.0 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
CHEMBL201584 145616 5 None None None Human 7.0 pKi = 7.0 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
4350931 333906 35 None None None Human 7.9 pKi = 7.9 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 333906 35 None None None Human 7.9 pKi = 7.9 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 333906 35 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 333906 35 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
42626289 294770 0 None None None Human 6.9 pKi = 6.9 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
CHEMBL393492 294770 0 None None None Human 6.9 pKi = 6.9 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
11566745 156363 0 None None None Human 8.6 pKi = 8.6 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 156363 0 None None None Human 8.6 pKi = 8.6 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
16090814 163015 0 None None None Human 8.6 pKi = 8.6 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 163015 0 None None None Human 8.6 pKi = 8.6 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11716449 278458 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 278458 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
5249956 145603 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 145603 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
11573628 156368 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 156368 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
11637457 145296 0 None None None Human 7.5 pKi = 7.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 145296 0 None None None Human 7.5 pKi = 7.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
9992499 145593 0 None None None Human 6.5 pKi = 6.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 145593 0 None None None Human 6.5 pKi = 6.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
11716438 278151 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 278151 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
44436300 295516 0 None None None Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL394110 295516 0 None None None Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
11558247 157089 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 157089 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
75201901 331247 26 None None None Human 8.3 pKi = 8.3 Functional
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 331247 26 None None None Human 8.3 pKi = 8.3 Functional
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
11536995 276865 0 None None None Human 7.3 pKi = 7.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 276865 0 None None None Human 7.3 pKi = 7.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
11718008 156958 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 156958 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
44408818 277455 0 None None None Human 8.1 pKi = 8.1 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 277455 0 None None None Human 8.1 pKi = 8.1 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
16090821 163261 0 None None None Human 7.1 pKi = 7.1 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 163261 0 None None None Human 7.1 pKi = 7.1 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
122324 421 19 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
6077 421 19 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
CHEMBL86931 421 19 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ligand		 Fold
selectivity		 # Tested
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3158 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
667468 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
956 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL101740 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB14750 18465 32 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1353 3909 69 None None None Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 3909 69 None None None Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 3909 69 None None None Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 3909 69 None None None Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 3909 69 None None None Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1613 4786 46 None None None Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 4786 46 None None None Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 4786 46 None None None Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 4786 46 None None None Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 4786 46 None None None Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
135398745 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1982 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
4585 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 5933 69 None None None Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
191 833 62 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 833 62 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 833 62 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 833 62 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 833 62 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2284 6466 25 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 6466 25 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 6466 25 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 6466 25 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 6466 25 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
1427 4113 43 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 4113 43 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 4113 43 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 4113 43 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 4113 43 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
85090335 354973 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 354973 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
168295528 385575 0 None None None Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 385575 0 None None None Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
85090318 353336 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 353336 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168290235 385513 0 None None None Human 4.6 pEC50 = 4.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 385513 0 None None None Human 4.6 pEC50 = 4.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
85090319 354482 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 354482 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090328 354896 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 354896 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090333 355154 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 355154 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090332 354588 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 354588 0 None None None Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
2030130 44828 24 None None None Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 44828 24 None None None Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090338 354629 0 None None None Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 354629 0 None None None Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168294767 385564 0 None None None Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 385564 0 None None None Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164612037 368668 0 None None None Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 368668 0 None None None Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
85090324 354562 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 354562 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090325 353636 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 353636 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090321 366195 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 366195 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090329 366069 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 366069 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
11938 4900 10 None None None Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 4900 10 None None None Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 4900 10 None None None Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090334 354497 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 354497 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090323 355760 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 355760 0 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
85090326 366156 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 366156 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090331 355302 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 355302 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090322 353350 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 353350 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090339 356132 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 356132 0 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
85090320 356380 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 356380 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
4901726 354667 7 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 354667 7 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
76284418 356144 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 356144 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
136326241 353319 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 353319 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090330 354934 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 354934 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090337 366627 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 366627 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
76284419 366596 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 366596 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
14202 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
3036864 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
3082393 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
5018 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
6603800 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
71451380 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
943 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
956 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
CHEMBL13668 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
CHEMBL2158641 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
CHEMBL62 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
CHEMBL63321 4235 21 None None None Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmc.2013.03.016
14202 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
3036864 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
3082393 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
5018 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
6603800 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
71451380 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
943 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
956 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL13668 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL2158641 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL62 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL63321 4235 21 None None None Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
5018 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
946 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
CHEMBL13668 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
5018 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
946 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
CHEMBL13668 8054 7 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
14202 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
3036864 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
3082393 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
5018 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
6603800 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
71451380 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
943 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
956 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL13668 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL2158641 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL62 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL63321 4235 21 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
10907460 24131 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 24131 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
11071079 220118 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 220118 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11730467 25309 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 25309 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11113605 24794 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 24794 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10918307 24287 0 None None None Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 514 5 1 7 2.6 CNC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)OCc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
CHEMBL114825 24287 0 None None None Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 514 5 1 7 2.6 CNC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)OCc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
11059058 24392 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 24392 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
11005810 24753 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 24753 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
10885636 220533 0 None None None Human 6.0 pIC50 = 6 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 220533 0 None None None Human 6.0 pIC50 = 6 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
164612037 368668 0 None -4 14 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 368668 0 None -4 14 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 385513 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 385513 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 385564 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 385564 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 385575 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 385575 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
11681599 156841 0 None 12 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 156841 0 None 12 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
14202 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
3036864 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
3082393 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
5018 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
6603800 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
71451380 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
943 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
956 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL13668 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL2158641 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL62 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
CHEMBL63321 4235 21 None -2 12 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.ejmech.2013.01.044
16665071 184192 0 None 7 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245764 184192 0 None 7 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
14202 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
3036864 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
3082393 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
5018 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
6603800 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
71451380 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
943 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
956 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
CHEMBL13668 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
CHEMBL2158641 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
CHEMBL62 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
CHEMBL63321 4235 21 None -2 12 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2020.127305
11465618 193817 22 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 193817 22 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
DB12188 193817 22 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
44439943 184159 0 None 1 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245570 184159 0 None 1 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
14202 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
3036864 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
3082393 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
5018 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
6603800 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
71451380 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
943 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
956 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL13668 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL2158641 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL62 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
CHEMBL63321 4235 21 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm8007618
1242 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
6603799 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
6852376 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
935 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
CHEMBL24077 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
CHEMBL284746 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
CHEMBL286080 7344 19 None 1 6 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2020.127305
11778580 138420 0 None 5 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 138420 0 None 5 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
16090814 163015 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 163015 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11393666 385531 0 None -1 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 385531 0 None -1 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
11595240 277476 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 277476 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11488247 448554 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 448554 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
46231784 462765 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 462765 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.ejmech.2024.116947
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.ejmech.2024.116947
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
11558055 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 145361 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11623343 278114 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 278114 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
10088113 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
1243 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
6604885 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
944 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
CHEMBL1473849 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
CHEMBL324017 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
CHEMBL416401 7354 32 None -2 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
10402378 138418 0 None 19 5 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 138418 0 None 19 5 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
122205438 274803 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 274803 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
122205438 274803 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1016/j.ejmech.2024.116947
CHEMBL3753266 274803 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1016/j.ejmech.2024.116947
46216855 447016 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 447016 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10088113 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
1243 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
6604885 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
944 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
CHEMBL1473849 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
CHEMBL324017 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
CHEMBL416401 7354 32 None -2 13 Human 8.7 pKi = 8.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.6019/CHEMBL5442175
46231925 462992 0 None -5 4 Human 8.0 pKi = 8 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 462992 0 None -5 4 Human 8.0 pKi = 8 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
45379370 21843 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 21843 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
6453963 143767 6 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1021/acs.jmedchem.4c00537
CHEMBL1962947 143767 6 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1021/acs.jmedchem.4c00537
11269330 463597 0 None -34 4 Human 8.0 pKi = 8.0 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 463597 0 None -34 4 Human 8.0 pKi = 8.0 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
135398745 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
1982 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
4585 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 5933 69 None -17 45 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
10947658 62361 0 None -912 16 Human 6.0 pKi = 6 Binding
Binding affinity against Dopamine receptor D5Binding affinity against Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 62361 0 None -912 16 Human 6.0 pKi = 6 Binding
Binding affinity against Dopamine receptor D5Binding affinity against Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
135398737 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2818 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL253391 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 1973 61 None -83 61 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2389 6775 83 None -229 45 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 6775 83 None -229 45 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 6775 83 None -229 45 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 6775 83 None -229 45 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 6775 83 None -229 45 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
155552185 348127 0 None -1819 16 Human 6.0 pKi = 6 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 348127 0 None -1819 16 Human 6.0 pKi = 6 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
154724609 350562 1 None -11 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 350562 1 None -11 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
45376872 142323 27 None None None Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 446 7 3 6 3.4 CCOC(=O)c1cc2cc(-c3cc(C(=O)NCc4ccc(C(=O)O)cc4)nn3C)ccc2[nH]1 10.6019/CHEMBL4507281
CHEMBL1939876 142323 27 None None None Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 446 7 3 6 3.4 CCOC(=O)c1cc2cc(-c3cc(C(=O)NCc4ccc(C(=O)O)cc4)nn3C)ccc2[nH]1 10.6019/CHEMBL4507281
56850410 142325 0 None None None Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 374 5 3 4 3.2 Cn1nc(C(=O)NCc2ccc(C(=O)O)cc2)cc1-c1ccc2[nH]ccc2c1 10.6019/CHEMBL4507281
CHEMBL1939880 142325 0 None None None Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 374 5 3 4 3.2 Cn1nc(C(=O)NCc2ccc(C(=O)O)cc2)cc1-c1ccc2[nH]ccc2c1 10.6019/CHEMBL4507281
72901200 238494 30 None -6918 33 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL3480577 238494 30 None -6918 33 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL4522773 478305 0 None -15 3 Human 5.0 pKi = 5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 385 2 2 4 4.9 CC1=C(C#N)[C@@H](c2ccc3[nH]nc(C)c3c2)C(C#N)=C(c2ccc(Cl)cc2)N1 10.6019/CHEMBL4507263
145969667 329878 0 None -41 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 329878 0 None -41 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
681 3019 53 None -67 20 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 3019 53 None -67 20 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 3019 53 None -67 20 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 3019 53 None -67 20 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 3019 53 None -67 20 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
21527771 142402 1 None -31 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 142402 1 None -31 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
172463952 388867 0 None -91 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 388867 0 None -91 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172463952 388867 0 None -91 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 388867 0 None -91 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
42611190 6416 21 None -4265 23 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
5802 6416 21 None -4265 23 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
CHEMBL1800685 6416 21 None -4265 23 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
44415593 161704 0 None -104 6 Human 7.0 pKi = 7.0 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 161704 0 None -104 6 Human 7.0 pKi = 7.0 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
242 971 74 None -112 38 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 971 74 None -112 38 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 971 74 None -112 38 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 971 74 None -112 38 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 971 74 None -112 38 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
154704368 350438 1 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 350438 1 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
126720252 329603 0 None -38 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 329603 0 None -38 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
130 7116 32 None -208 13 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
3378093 7116 32 None -208 13 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
CHEMBL281350 7116 32 None -208 13 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
11566745 156363 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 156363 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
154704418 350550 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 350550 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
11408135 251147 0 None -245 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL363406 251147 0 None -245 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
5249956 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
5249956 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201525 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
5249956 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 145603 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
56594534 142843 0 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 142843 0 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
56597938 8555 11 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 8555 11 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 8555 11 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
164618319 367902 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4848838 367902 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
122181333 240467 0 None -7762 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 240467 0 None -7762 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
154725276 350259 1 None -40 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 350259 1 None -40 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
11335419 139387 0 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 139387 0 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
21533446 142401 0 None -24 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 142401 0 None -24 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
44436302 181453 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238917 181453 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
44436302 181453 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238917 181453 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmc.2007.06.002
681 3019 53 None -67 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 3019 53 None -67 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 3019 53 None -67 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 3019 53 None -67 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 3019 53 None -67 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
11573806 157083 0 None -6 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 157083 0 None -6 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
11151831 27379 0 None None None Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1190453 27379 0 None None None Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
154706513 350549 1 None -18 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 350549 1 None -18 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
53324045 119869 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 119869 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
3038495 1458 35 None -1288 27 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 1458 35 None -1288 27 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 1458 35 None -1288 27 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
1242 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
6603799 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
6852376 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
935 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
CHEMBL24077 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
CHEMBL284746 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
CHEMBL286080 7344 19 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
487 7383 17 None -3235 29 Human 5.9 pKi = 5.9 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442175
60602 7383 17 None -3235 29 Human 5.9 pKi = 5.9 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442175
CHEMBL405355 7383 17 None -3235 29 Human 5.9 pKi = 5.9 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442175
DB09239 7383 17 None -3235 29 Human 5.9 pKi = 5.9 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442175
2080 352858 63 None 1 22 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
33630 352858 63 None 1 22 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 352858 63 None 1 22 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
DB13791 352858 63 None 1 22 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
164609730 368399 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4856060 368399 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
11154178 446093 0 None -64 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
CHEMBL596824 446093 0 None -64 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
177380472 391132 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 329 2 2 5 2.9 COC1=CC2C[C@@H]3c4cc(O)c(OC)cc4CCN3CC2C=C1O 10.1021/acs.jmedchem.4c00537
CHEMBL5563974 391132 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 329 2 2 5 2.9 COC1=CC2C[C@@H]3c4cc(O)c(OC)cc4CCN3CC2C=C1O 10.1021/acs.jmedchem.4c00537
122191607 251793 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 251793 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
137654675 314501 0 None -3388 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 314501 0 None -3388 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
11739113 27356 0 None None None Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1190331 27356 0 None None None Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
57391216 142414 0 None -66 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 142414 0 None -66 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
11716449 278458 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 278458 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
164609539 367711 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4845850 367711 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
145988180 330128 0 None -12 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 330128 0 None -12 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
164585473 367871 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to D5 receptor (unknown origin)Binding affinity to D5 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 367871 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to D5 receptor (unknown origin)Binding affinity to D5 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44209480 142416 1 None -1318 11 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 142416 1 None -1318 11 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
1353 3909 69 None -42 49 Human 6.8 pKi = 6.8 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.4c00537
3559 3909 69 None -42 49 Human 6.8 pKi = 6.8 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.4c00537
86 3909 69 None -42 49 Human 6.8 pKi = 6.8 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.4c00537
CHEMBL54 3909 69 None -42 49 Human 6.8 pKi = 6.8 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.4c00537
DB00502 3909 69 None -42 49 Human 6.8 pKi = 6.8 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.4c00537
11637457 145296 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 145296 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
11637457 145296 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1016/j.ejmech.2024.116947
CHEMBL201093 145296 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1016/j.ejmech.2024.116947
228 919 20 None -6 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
33 919 20 None -6 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
6005 919 20 None -6 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
CHEMBL53 919 20 None -6 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
DB00714 919 20 None -6 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
3246443 81141 0 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 81141 0 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
137636066 312157 0 None -9549 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 312157 0 None -9549 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11439436 27059 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188091 27059 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
46227284 433055 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
CHEMBL593394 433055 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
90644071 221530 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 221530 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
45379377 21777 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
CHEMBL1086790 21777 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
44591134 350165 0 None -125 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459373 350165 0 None -125 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
72164182 182943 0 None -25 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 182943 0 None -25 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
150860015 387400 0 None -7 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 440 10 2 6 4.9 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2ccc(Cl)c3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
CHEMBL5395401 387400 0 None -7 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 440 10 2 6 4.9 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2ccc(Cl)c3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
172450959 388056 0 None -51 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 388056 0 None -51 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
154703647 350334 1 None -28 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 350334 1 None -28 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
14708665 193602 18 None -1 11 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
6603820 193602 18 None -1 11 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 193602 18 None -1 11 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL43345 193602 18 None -1 11 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
DB16139 193602 18 None -1 11 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
10200496 174593 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 174593 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
242 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 971 74 None -112 38 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
163198500 369667 4 None 3 2 Human 5.8 pKi = 5.8 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
CHEMBL4875858 369667 4 None 3 2 Human 5.8 pKi = 5.8 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
137655795 314452 0 None -6309 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 314452 0 None -6309 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
137660046 315188 0 None -22387 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 315188 0 None -22387 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
11324023 27076 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188254 27076 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11416811 27089 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188384 27089 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11438636 27378 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)C[C@@H](N(C)C)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL1190452 27378 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)C[C@@H](N(C)C)[C@@H]2c1ccccc1 10.1021/jm040889k
11818686 28143 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N)C2 10.1021/jm040889k
CHEMBL1196231 28143 0 None None None Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N)C2 10.1021/jm040889k
85658088 329915 0 None -5 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 329915 0 None -5 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
172450959 388056 0 None -51 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 388056 0 None -51 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader methodDisplacement of [3H]N-methylspiperone from Dopamine D5 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
44436300 295516 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL394110 295516 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
44436300 295516 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL394110 295516 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
17755866 280028 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 280028 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
180 829 44 None -25 32 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
200 829 44 None -25 32 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
2160 829 44 None -25 32 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL629 829 44 None -25 32 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
DB00321 829 44 None -25 32 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
44436305 310454 0 None -23 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 430 6 0 5 4.0 O=c1c2ccccc2ncn1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL398813 310454 0 None -23 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 430 6 0 5 4.0 O=c1c2ccccc2ncn1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
11464115 135882 0 None -89 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL191815 135882 0 None -89 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
2726 1895 54 None -26 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
621 1895 54 None -26 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
83 1895 54 None -26 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL71 1895 54 None -26 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
DB00477 1895 54 None -26 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
154705520 350229 1 None -114 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 350229 1 None -114 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
76314268 216104 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 216104 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
72164180 182938 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420772 182938 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
11134444 181452 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238916 181452 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
11134444 181452 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238916 181452 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
57401819 142406 0 None -229 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 142406 0 None -229 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
76314268 216104 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 216104 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
46227325 445478 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
CHEMBL596179 445478 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
11358377 465908 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
CHEMBL610449 465908 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
129989 933 31 None -457 11 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
8584 933 31 None -457 11 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
CHEMBL43383 933 31 None -457 11 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
154726793 350202 1 None -61 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 350202 1 None -61 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
46227317 445726 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 445726 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
228 919 20 None -6 24 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting methodBinding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acs.jmedchem.4c00537
33 919 20 None -6 24 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting methodBinding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acs.jmedchem.4c00537
6005 919 20 None -6 24 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting methodBinding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acs.jmedchem.4c00537
CHEMBL53 919 20 None -6 24 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting methodBinding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acs.jmedchem.4c00537
DB00714 919 20 None -6 24 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting methodBinding affinity to human recombinant D5 receptor expressed in CHO cells assessed as inhibition constant incubated for 60 mins by liquid scintillation counting method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acs.jmedchem.4c00537
44436306 197513 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL268371 197513 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
137645830 313738 0 None -478 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 313738 0 None -478 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
11449266 28194 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)C[C@@H](N)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL1196658 28194 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)C[C@@H](N)[C@@H]2c1ccccc1 10.1021/jm040889k
11449669 28195 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196659 28195 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11210215 28245 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1197038 28245 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
76336022 216053 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 216053 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
11775107 327622 0 None -588 3 Rat 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL426629 327622 0 None -588 3 Rat 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
76336022 216053 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 216053 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
9893924 19088 27 None -81 22 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442175
CHEMBL103769 19088 27 None -81 22 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442175
135398737 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
2818 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
38 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
722 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL253391 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL42 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
DB00363 1973 61 None -83 61 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
75306277 218830 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 218830 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
90644062 221522 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 221522 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
154727843 350401 1 None -17 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 350401 1 None -17 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
107930 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
14787976 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL56666 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
107930 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
14787976 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL56666 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 3147 31 None 1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
46231927 463820 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 463820 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10088113 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
1243 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
6604885 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
944 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
CHEMBL1473849 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
CHEMBL324017 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
CHEMBL416401 7354 32 None -2 13 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127053
45379369 21842 0 None 1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 21842 0 None 1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
46231926 448193 0 None -12 4 Human 8.6 pKi = 8.6 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 448193 0 None -12 4 Human 8.6 pKi = 8.6 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
14202 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
3036864 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
3082393 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
5018 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
6603800 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
71451380 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
943 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
956 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
CHEMBL13668 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
CHEMBL2158641 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
CHEMBL62 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
CHEMBL63321 4235 21 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1016/j.bmcl.2009.12.100
11416809 27069 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188198 27069 0 None None None Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
23653176 182015 0 None 4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 383 6 0 3 3.8 O=C1Cc2ccccc2N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL239917 182015 0 None 4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 383 6 0 3 3.8 O=C1Cc2ccccc2N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
763625 182941 5 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420775 182941 5 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
3038495 1458 35 None -1288 27 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
7625 1458 35 None -1288 27 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
CHEMBL25236 1458 35 None -1288 27 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
1212 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/acs.jmedchem.4c00537
204 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/acs.jmedchem.4c00537
3372 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/acs.jmedchem.4c00537
CHEMBL726 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/acs.jmedchem.4c00537
DB00623 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/acs.jmedchem.4c00537
1212 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
204 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
3372 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
CHEMBL726 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
DB00623 3415 38 None -7 41 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
164615845 368488 0 None -2 6 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
CHEMBL4857492 368488 0 None -2 6 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
164623060 369447 0 None None None Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 325 1 0 3 4.0 CC(C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4872572 369447 0 None None None Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 325 1 0 3 4.0 CC(C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
122177644 239820 0 None -17378 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 239820 0 None -17378 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
154725234 350261 1 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 350261 1 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
90644062 221522 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 221522 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
46231924 448192 0 None -5 4 Human 7.7 pKi = 7.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 448192 0 None -5 4 Human 7.7 pKi = 7.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
154705128 350260 1 None -151 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 350260 1 None -151 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
156020558 351971 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4647167 351971 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
11558247 157089 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 157089 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
145969667 329878 0 None -41 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 329878 0 None -41 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
681 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.4c00537
940 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.4c00537
947 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.4c00537
CHEMBL59 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.4c00537
DB00988 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.4c00537
44436301 181451 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238915 181451 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
44436301 181451 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238915 181451 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
135398737 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
2818 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL253391 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 1973 61 None -83 61 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
44209472 142418 1 None -1318 11 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 142418 1 None -1318 11 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
181743 346764 4 None -1202 22 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH233930 from human dopamine D5 receptorDisplacement of [3H]SCH233930 from human dopamine D5 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 346764 4 None -1202 22 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH233930 from human dopamine D5 receptorDisplacement of [3H]SCH233930 from human dopamine D5 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
122177641 239817 0 None -38018 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 239817 0 None -38018 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
161665 337100 30 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL448891 337100 30 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
681 3019 53 None -67 20 Human 5.6 pKi = 5.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm040889k
940 3019 53 None -67 20 Human 5.6 pKi = 5.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm040889k
947 3019 53 None -67 20 Human 5.6 pKi = 5.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm040889k
CHEMBL59 3019 53 None -67 20 Human 5.6 pKi = 5.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm040889k
DB00988 3019 53 None -67 20 Human 5.6 pKi = 5.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm040889k
1242 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
6603799 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
6852376 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
935 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL24077 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL284746 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL286080 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
76325152 216046 0 None -251 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 216046 0 None -251 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
1242 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
6603799 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
6852376 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
935 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL24077 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL284746 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
CHEMBL286080 7344 19 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmcl.2013.12.024
156015018 351517 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4640497 351517 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
122177643 239819 0 None -15848 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 239819 0 None -15848 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
90644061 221521 0 None -2344 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 221521 0 None -2344 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
11610526 4648 42 None -74 7 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 377 4 1 4 3.3 CN1CCC(CC1)C(=O)c1cccc(n1)NC(=O)c1c(F)cc(cc1F)F 10.6019/CHEMBL5442175
3928 4648 42 None -74 7 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 377 4 1 4 3.3 CN1CCC(CC1)C(=O)c1cccc(n1)NC(=O)c1c(F)cc(cc1F)F 10.6019/CHEMBL5442175
5351 4648 42 None -74 7 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 377 4 1 4 3.3 CN1CCC(CC1)C(=O)c1cccc(n1)NC(=O)c1c(F)cc(cc1F)F 10.6019/CHEMBL5442175
CHEMBL3039520 4648 42 None -74 7 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 377 4 1 4 3.3 CN1CCC(CC1)C(=O)c1cccc(n1)NC(=O)c1c(F)cc(cc1F)F 10.6019/CHEMBL5442175
DB11732 4648 42 None -74 7 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 377 4 1 4 3.3 CN1CCC(CC1)C(=O)c1cccc(n1)NC(=O)c1c(F)cc(cc1F)F 10.6019/CHEMBL5442175
90644061 221521 0 None -2344 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 221521 0 None -2344 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
11223708 327627 0 None -16 3 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL427173 327627 0 None -16 3 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
46231848 448005 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 448005 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
1353 3909 69 None -42 49 Human 6.6 pKi = 6.6 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 3909 69 None -42 49 Human 6.6 pKi = 6.6 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 3909 69 None -42 49 Human 6.6 pKi = 6.6 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 3909 69 None -42 49 Human 6.6 pKi = 6.6 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 3909 69 None -42 49 Human 6.6 pKi = 6.6 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
11246806 27268 0 None None None Human 4.6 pKi = 4.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 327 6 1 2 4.7 CCCN(CCC)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1189734 27268 0 None None None Human 4.6 pKi = 4.6 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 327 6 1 2 4.7 CCCN(CCC)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11522476 156193 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 156193 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
156017805 351757 0 None -5 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4643886 351757 0 None -5 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
25212275 348472 0 None -6309 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL455288 348472 0 None -6309 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
25212276 373163 0 None -741 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517244 373163 0 None -741 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
1530 4450 49 None -2951 24 Human 5.6 pKi = 5.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
3827 4450 49 None -2951 24 Human 5.6 pKi = 5.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
7206 4450 49 None -2951 24 Human 5.6 pKi = 5.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
CHEMBL534 4450 49 None -2951 24 Human 5.6 pKi = 5.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
DB00920 4450 49 None -2951 24 Human 5.6 pKi = 5.6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
57391307 142409 0 None -389 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 142409 0 None -389 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
146025727 336217 0 None 4 27 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 336217 0 None 4 27 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
11316709 327725 0 None -323 3 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL434532 327725 0 None -323 3 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
44591099 350155 0 None -977 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459350 350155 0 None -977 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
76325156 212893 0 None -12302 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 212893 0 None -12302 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
76325156 212893 0 None -12302 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 212893 0 None -12302 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
164606105 386528 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine 5 receptor (unknown origin)Binding affinity to dopamine 5 receptor (unknown origin)
ChEMBL 279 1 0 3 3.3 O=[N+]([O-])C1=Cc2cc(Cl)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2022.128981
CHEMBL5279730 386528 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine 5 receptor (unknown origin)Binding affinity to dopamine 5 receptor (unknown origin)
ChEMBL 279 1 0 3 3.3 O=[N+]([O-])C1=Cc2cc(Cl)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2022.128981
46869265 40147 0 None -13 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 40147 0 None -13 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
122181326 240460 0 None -933 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 240460 0 None -933 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
57401820 142407 0 None -323 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 142407 0 None -323 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
42611190 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
5802 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
CHEMBL1800685 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
42611190 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
5802 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
CHEMBL1800685 6416 21 None -4265 23 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
147326216 389070 0 None -28 15 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 424 10 2 6 4.3 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
CHEMBL5431371 389070 0 None -28 15 Human 5.6 pKi = 5.6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 424 10 2 6 4.3 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
CHEMBL4566600 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL4507292
CHEMBL4745071 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL4507292
CHEMBL4566600 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD5Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
CHEMBL4745071 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD5Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
145967572 329846 0 None -56 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 329846 0 None -56 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4566600 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL4507292
CHEMBL4745071 478333 0 None -1 6 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 489 4 2 2 7.7 Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL4507292
76325152 216046 0 None -251 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 216046 0 None -251 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
115237 118408 70 None -5 26 Human 7.5 pKi = 7.5 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O 10.1021/acs.jmedchem.4c00537
4137 118408 70 None -5 26 Human 7.5 pKi = 7.5 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O 10.1021/acs.jmedchem.4c00537
CHEMBL1621 118408 70 None -5 26 Human 7.5 pKi = 7.5 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O 10.1021/acs.jmedchem.4c00537
DB01267 118408 70 None -5 26 Human 7.5 pKi = 7.5 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O 10.1021/acs.jmedchem.4c00537
122181329 240463 0 None -9332 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 240463 0 None -9332 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
10531 2923 15 None -7762 30 Human 5.5 pKi = 5.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.6019/CHEMBL5442175
121 2923 15 None -7762 30 Human 5.5 pKi = 5.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.6019/CHEMBL5442175
888 2923 15 None -7762 30 Human 5.5 pKi = 5.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.6019/CHEMBL5442175
CHEMBL1732 2923 15 None -7762 30 Human 5.5 pKi = 5.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.6019/CHEMBL5442175
DB00320 2923 15 None -7762 30 Human 5.5 pKi = 5.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.6019/CHEMBL5442175
44591135 373272 0 None -190 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517407 373272 0 None -190 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
122205437 274715 0 None 7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 274715 0 None 7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
122205437 274715 0 None 7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1016/j.ejmech.2024.116947
CHEMBL3752512 274715 0 None 7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1016/j.ejmech.2024.116947
6603703 427 11 None 1 12 Human 8.5 pKi = 8.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442175
9637 427 11 None 1 12 Human 8.5 pKi = 8.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442175
CHEMBL291143 427 11 None 1 12 Human 8.5 pKi = 8.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442175
11486421 461965 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL603485 461965 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
46231846 462769 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 462769 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231849 463208 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 463208 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 447215 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 447215 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44439942 298501 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
CHEMBL396560 298501 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
46231782 447808 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 447808 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
46231541 445894 0 None -4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL596622 445894 0 None -4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
10088113 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
1243 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
6604885 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
944 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
CHEMBL1473849 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
CHEMBL324017 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
CHEMBL416401 7354 32 None -2 13 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2020.127305
164609519 367761 0 None -251 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 367761 0 None -251 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
172444635 387763 0 None -1905 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 488 10 2 5 4.4 COc1ccc(-c2ccccc2)c(CNC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/acs.jmedchem.3c00537
CHEMBL5403204 387763 0 None -1905 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 488 10 2 5 4.4 COc1ccc(-c2ccccc2)c(CNC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/acs.jmedchem.3c00537
137646281 313693 0 None -6918 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 313693 0 None -6918 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
72301 365865 50 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL487182 365865 50 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
DB12093 365865 50 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
10801923 351700 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4642805 351700 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
44415690 161596 0 None -14 6 Human 7.5 pKi = 7.5 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 161596 0 None -14 6 Human 7.5 pKi = 7.5 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
44439944 298505 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
CHEMBL396561 298505 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
145968810 329948 0 None -33 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 329948 0 None -33 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
42626293 297777 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 349 6 0 3 3.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL395933 297777 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 349 6 0 3 3.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
11186895 178375 31 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
CHEMBL2334885 178375 31 None -7 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
17755991 298929 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 298929 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
90644063 221523 0 None -138 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 221523 0 None -138 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
11394805 28229 0 None None None Human 4.5 pKi = 4.5 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 341 7 0 2 5.0 CCCN(CCC)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196936 28229 0 None None None Human 4.5 pKi = 4.5 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 341 7 0 2 5.0 CCCN(CCC)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
57401706 142417 0 None -562 11 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 142417 0 None -562 11 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
90644063 221523 0 None -138 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 221523 0 None -138 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44436307 182557 0 None 19 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 383 6 0 3 3.9 O=C1c2ccccc2CN1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL240995 182557 0 None 19 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 383 6 0 3 3.9 O=C1c2ccccc2CN1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
10667433 295478 0 None -10 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 379 7 0 4 3.2 COc1ccccc1N1CCN(CCCCN2C(=O)Cc3ccccc32)CC1 10.1016/j.bmc.2007.06.002
CHEMBL394080 295478 0 None -10 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 379 7 0 4 3.2 COc1ccccc1N1CCN(CCCCN2C(=O)Cc3ccccc32)CC1 10.1016/j.bmc.2007.06.002
172458734 388823 0 None -6165 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 458 9 2 4 4.4 COc1ccccc1N1CCN(CCCNC(=O)NCc2ccccc2-c2ccccc2)CC1 10.1021/acs.jmedchem.3c00537
CHEMBL5425252 388823 0 None -6165 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 458 9 2 4 4.4 COc1ccccc1N1CCN(CCCNC(=O)NCc2ccccc2-c2ccccc2)CC1 10.1021/acs.jmedchem.3c00537
154 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
1621 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
638252 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 4804 8 None -25 23 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
155515982 334571 1 None -1348 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 334571 1 None -1348 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
164626655 369859 0 None -100 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 369859 0 None -100 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
137636498 312120 0 None -1479 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 312120 0 None -1479 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11978813 1488 62 None -371 28 Human 6.5 pKi = 6.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442175
5014 1488 62 None -371 28 Human 6.5 pKi = 6.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442175
7672 1488 62 None -371 28 Human 6.5 pKi = 6.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442175
CHEMBL2105760 1488 62 None -371 28 Human 6.5 pKi = 6.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442175
DB09128 1488 62 None -371 28 Human 6.5 pKi = 6.5 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442175
76321556 216052 0 None -363 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 216052 0 None -363 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
76321556 216052 0 None -363 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 216052 0 None -363 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
168510312 387325 2 None -218 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 520 9 2 4 6.4 COc1ccccc1N1CCN(CCCNC(=O)Nc2ccccc2-c2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.3c00537
CHEMBL5394229 387325 2 None -218 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 520 9 2 4 6.4 COc1ccccc1N1CCN(CCCNC(=O)Nc2ccccc2-c2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.3c00537
154703824 350589 1 None -1348 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 350589 1 None -1348 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
763774 182942 3 None -16 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420776 182942 3 None -16 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
76321554 216075 0 None -2290 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 216075 0 None -2290 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
122191605 251791 0 None -181 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 251791 0 None -181 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
9992499 145593 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 145593 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
2993172 255131 3 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 255131 3 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
10476504 67103 1 None -154 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 67103 1 None -154 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
10378389 461700 0 None -8128 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 461700 0 None -8128 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
76321554 216075 0 None -2290 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 216075 0 None -2290 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
44415569 330796 0 None -23 6 Human 7.4 pKi = 7.4 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 330796 0 None -23 6 Human 7.4 pKi = 7.4 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
75201901 331247 26 None 1 24 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 331247 26 None 1 24 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
1353 3909 69 None -42 49 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 3909 69 None -42 49 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 3909 69 None -42 49 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 3909 69 None -42 49 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 3909 69 None -42 49 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
44408818 277455 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
CHEMBL380330 277455 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
122180956 240369 0 None -380 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 240369 0 None -380 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
137635364 312184 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 312184 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
57393083 142413 0 None -616 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 142413 0 None -616 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
10378389 461700 0 None -8128 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 461700 0 None -8128 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
56594533 142841 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949726 142841 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
172458161 388726 0 None -1862 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 562 15 2 7 4.7 COCCOCCOc1ccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c(-c2ccccc2)c1 10.1021/acs.jmedchem.3c00537
CHEMBL5422870 388726 0 None -1862 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 562 15 2 7 4.7 COCCOCCOc1ccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c(-c2ccccc2)c1 10.1021/acs.jmedchem.3c00537
3929516 212927 4 None -66 17 Human 6.4 pKi = 6.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 343 4 0 2 4.7 CN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.6019/CHEMBL5442175
CHEMBL317757 212927 4 None -66 17 Human 6.4 pKi = 6.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 343 4 0 2 4.7 CN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.6019/CHEMBL5442175
132060461 387774 0 None -199 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 421 6 0 4 4.9 CCCN1CCN(c2ccc3c(c2)C(N(C)C(=O)OCc2ccccc2)CCC3)CC1 10.1016/j.ejmech.2022.114696
CHEMBL5403404 387774 0 None -199 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to human dopamine D5 receptor assessed as inhibition constantBinding affinity to human dopamine D5 receptor assessed as inhibition constant
ChEMBL 421 6 0 4 4.9 CCCN1CCN(c2ccc3c(c2)C(N(C)C(=O)OCc2ccccc2)CCC3)CC1 10.1016/j.ejmech.2022.114696
168269421 373063 0 None -26 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from human D5 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D5 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 373063 0 None -26 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from human D5 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D5 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
6917970 7498 42 None 1 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 7498 42 None 1 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 7498 42 None 1 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
56589560 142840 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 142840 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
17756101 198844 0 None 4 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 198844 0 None 4 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
46231995 463811 0 None -7 4 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 463811 0 None -7 4 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11573628 156368 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 156368 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
10472143 232141 0 None -891 16 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 232141 0 None -891 16 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
154703922 350258 1 None -1995 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 350258 1 None -1995 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
126609223 387119 0 None -16 2 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 487 9 2 7 1.6 CCn1c(CNC(=O)c2nc(Cl)cnc2N)[n+](CC)c2ccc(C(=O)N(C)CCN(C)C)cc21 10.6019/CHEMBL5303762
CHEMBL5315634 387119 0 None -16 2 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 487 9 2 7 1.6 CCn1c(CNC(=O)c2nc(Cl)cnc2N)[n+](CC)c2ccc(C(=O)N(C)CCN(C)C)cc21 10.6019/CHEMBL5303762
126609223 387119 0 None -16 2 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 487 9 2 7 1.6 CCn1c(CNC(=O)c2nc(Cl)cnc2N)[n+](CC)c2ccc(C(=O)N(C)CCN(C)C)cc21 10.6019/CHEMBL5303762
CHEMBL5315634 387119 0 None -16 2 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of D5GPCRScan assay: inhibition of D5
ChEMBL 487 9 2 7 1.6 CCn1c(CNC(=O)c2nc(Cl)cnc2N)[n+](CC)c2ccc(C(=O)N(C)CCN(C)C)cc21 10.6019/CHEMBL5303762
13373172 443318 0 None 3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 443318 0 None 3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
44414299 276551 0 None -19 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 495 9 0 4 6.6 CCN(CC)CCCOc1cccc(N2C(=O)/C(=N/c3cccc(C(F)(F)F)c3)c3ccccc32)c1 10.1016/j.bmcl.2006.05.025
CHEMBL378825 276551 0 None -19 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 495 9 0 4 6.6 CCN(CC)CCCOc1cccc(N2C(=O)/C(=N/c3cccc(C(F)(F)F)c3)c3ccccc32)c1 10.1016/j.bmcl.2006.05.025
2402 6855 40 None -79 14 Human 4.4 pKi = 4.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 6855 40 None -79 14 Human 4.4 pKi = 4.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 6855 40 None -79 14 Human 4.4 pKi = 4.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 6855 40 None -79 14 Human 4.4 pKi = 4.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 6855 40 None -79 14 Human 4.4 pKi = 4.4 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
135409453 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
226 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
2579 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
5362436 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
CHEMBL76370 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
DB01079 8225 26 None -524 19 Human 5.4 pKi = 5.4 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.6019/CHEMBL5442175
2150 139247 20 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
7077 139247 20 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 139247 20 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
DB11160 139247 20 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
57403525 142400 0 None -275 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 142400 0 None -275 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
156012196 351284 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1021/acs.jmedchem.4c00537
CHEMBL4637246 351284 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1021/acs.jmedchem.4c00537
156012196 351284 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4637246 351284 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to human D5 receptorBinding affinity to human D5 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
11716438 278151 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 278151 0 None -8 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
137640189 312865 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 312865 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
164614469 368090 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 341 1 0 3 3.9 C[Si](C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4851349 368090 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 341 1 0 3 3.9 C[Si](C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
154726353 350292 1 None -371 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 350292 1 None -371 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1634 163834 36 None -20 21 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
4011 163834 36 None -20 21 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
CHEMBL21731 163834 36 None -20 21 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
DB00934 163834 36 None -20 21 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
44396220 253433 0 None -1 6 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 253433 0 None -1 6 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
11212939 135884 0 None -45 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL192439 135884 0 None -45 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
145988693 331960 0 None -17 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 331960 0 None -17 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
145969934 329955 0 None -39 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 329955 0 None -39 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
155770281 351683 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D5 receptor (unknown origin)Binding affinity to dopamine D5 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4642592 351683 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D5 receptor (unknown origin)Binding affinity to dopamine D5 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
156011597 351329 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4637938 351329 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
172438970 387646 0 None -776 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 444 8 2 4 4.7 COc1ccccc1N1CCN(CCCNC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/acs.jmedchem.3c00537
CHEMBL5400232 387646 0 None -776 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells assessed as inhibition constant by competition binding assay
ChEMBL 444 8 2 4 4.7 COc1ccccc1N1CCN(CCCNC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/acs.jmedchem.3c00537
76325150 216094 0 None -4897 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 216094 0 None -4897 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
156017431 351712 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643069 351712 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
76325150 216094 0 None -4897 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 216094 0 None -4897 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
130442572 336435 0 None 3 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 336435 0 None 3 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
156018764 351729 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643426 351729 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
156018236 351840 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4645139 351840 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
1353 3909 69 None -42 49 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 3909 69 None -42 49 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 3909 69 None -42 49 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 3909 69 None -42 49 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 3909 69 None -42 49 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
122177642 239818 0 None -21877 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 239818 0 None -21877 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
156014482 351164 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635423 351164 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
156010755 351095 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4633950 351095 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
5074 6777 51 None -776 31 Human 6.3 pKi = 6.3 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.6019/CHEMBL5442175
97 6777 51 None -776 31 Human 6.3 pKi = 6.3 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.6019/CHEMBL5442175
CHEMBL267777 6777 51 None -776 31 Human 6.3 pKi = 6.3 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.6019/CHEMBL5442175
DB12693 6777 51 None -776 31 Human 6.3 pKi = 6.3 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.6019/CHEMBL5442175
44439945 184160 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245571 184160 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
168280742 374156 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D5R in transfected cellsCompetitive binding affinity to human D5R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 374156 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D5R in transfected cellsCompetitive binding affinity to human D5R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
11452916 449961 0 None -7 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600986 449961 0 None -7 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
44275670 26262 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4 versus hD2, hD3 receptorBinding affinity against human Dopamine receptor D4 versus hD2, hD3 receptor
ChEMBL 457 8 2 5 3.7 COc1cccc(CN2CC[C@H](NC(=O)c3cc(Cl)c(NC(=O)C4CC4)cc3OC)C2)c1 10.1021/jm030480f
CHEMBL1183144 26262 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4 versus hD2, hD3 receptorBinding affinity against human Dopamine receptor D4 versus hD2, hD3 receptor
ChEMBL 457 8 2 5 3.7 COc1cccc(CN2CC[C@H](NC(=O)c3cc(Cl)c(NC(=O)C4CC4)cc3OC)C2)c1 10.1021/jm030480f
6917970 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.4c00537
8370 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.4c00537
CHEMBL487387 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.4c00537
11235174 447027 0 None -11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL597909 447027 0 None -11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11374299 448348 0 None -11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599282 448348 0 None -11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
156020547 352078 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4649012 352078 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
44436304 181271 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 396 6 0 5 3.7 O=c1c2ccccc2ncn1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238718 181271 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 396 6 0 5 3.7 O=c1c2ccccc2ncn1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2007.06.002
44427970 299235 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 299235 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
56593482 8557 12 None -467 9 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 8557 12 None -467 9 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 8557 12 None -467 9 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
71528209 177848 1 None -812 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 177848 1 None -812 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
53325242 119868 0 None -2 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 119868 0 None -2 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
44415689 276442 0 None -58 6 Human 7.3 pKi = 7.3 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 276442 0 None -58 6 Human 7.3 pKi = 7.3 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
17756102 177023 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 177023 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
44408818 277455 0 None -9 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL380330 277455 0 None -9 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm070388+
44408818 277455 0 None -9 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 277455 0 None -9 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
11441173 28203 0 None None None Human 4.3 pKi = 4.3 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 327 6 1 2 4.7 CCCN(CCC)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196699 28203 0 None None None Human 4.3 pKi = 4.3 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 327 6 1 2 4.7 CCCN(CCC)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
17755999 280029 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 280029 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
154725813 350491 1 None -213 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 350491 1 None -213 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
137643132 313932 0 None -4786 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 313932 0 None -4786 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
154703541 350268 1 None -24 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 350268 1 None -24 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
21509921 214176 0 None -56 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 214176 0 None -56 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
154705296 350362 1 None -134 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 350362 1 None -134 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
44415704 161617 0 None -19 6 Human 7.2 pKi = 7.2 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 161617 0 None -19 6 Human 7.2 pKi = 7.2 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
1353 3909 69 None -42 49 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 3909 69 None -42 49 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 3909 69 None -42 49 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 3909 69 None -42 49 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 3909 69 None -42 49 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
137635685 311931 0 None -199 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 311931 0 None -199 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
21509921 214176 0 None -56 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 214176 0 None -56 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
154704705 350294 1 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 350294 1 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
11121216 63789 0 None -295 14 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 63789 0 None -295 14 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
11198948 27965 0 None None None Human 5.2 pKi = 5.2 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 2 1 2 3.2 CN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1194996 27965 0 None None None Human 5.2 pKi = 5.2 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 2 1 2 3.2 CN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
46232066 462320 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 462320 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
171347340 386688 0 None None None Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine 5 receptor (unknown origin)Binding affinity to dopamine 5 receptor (unknown origin)
ChEMBL 375 2 1 4 3.5 O=[N+]([O-])C1=Cc2cc(C#Cc3ccc(CO)cc3)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2022.128981
CHEMBL5283362 386688 0 None None None Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine 5 receptor (unknown origin)Binding affinity to dopamine 5 receptor (unknown origin)
ChEMBL 375 2 1 4 3.5 O=[N+]([O-])C1=Cc2cc(C#Cc3ccc(CO)cc3)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2022.128981
145970938 330058 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 330058 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
154705884 350332 1 None -190 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 350332 1 None -190 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
56597938 8555 11 None -1380 9 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 8555 11 None -1380 9 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 8555 11 None -1380 9 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
21171 365873 31 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 365873 31 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
11406143 138425 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
CHEMBL184073 138425 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
145986752 332067 0 None -1 17 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 332067 0 None -1 17 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
3038495 1458 35 None -501 27 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
7625 1458 35 None -501 27 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
CHEMBL25236 1458 35 None -501 27 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
145969667 329878 0 None -41 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 329878 0 None -41 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145967904 330004 0 None -5 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 330004 0 None -5 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
56594402 142842 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 334 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1C(=O)O 10.1021/jm200676f
CHEMBL1949727 142842 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 334 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1C(=O)O 10.1021/jm200676f
70607606 351156 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635277 351156 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
11247757 270429 0 None -741 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL371200 270429 0 None -741 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
17756213 296381 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 296381 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
44415672 161632 0 None -5 6 Human 8.2 pKi = 8.2 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 161632 0 None -5 6 Human 8.2 pKi = 8.2 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
46231768 431358 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL591685 431358 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
25142456 155194 1 None -3 9 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D5 receptorBinding affinity to human cloned dopamine D5 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 155194 1 None -3 9 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D5 receptorBinding affinity to human cloned dopamine D5 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
11223303 449964 0 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600987 449964 0 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
46231847 448175 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 448175 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
4350931 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
4350931 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.ejmech.2024.116947
CHEMBL441618 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to dopamine D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.ejmech.2024.116947
4350931 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
4350931 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL441618 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
4350931 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 333906 35 None -123 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
46231845 449094 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 449094 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
122177645 239821 0 None -3311 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 239821 0 None -3311 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
122181330 240464 0 None -8128 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 240464 0 None -8128 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
22475020 196360 21 None -177 7 Human 6.2 pKi = 6.2 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.6019/CHEMBL5442175
CHEMBL259656 196360 21 None -177 7 Human 6.2 pKi = 6.2 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.6019/CHEMBL5442175
11301268 28217 0 None None None Human 4.2 pKi = 4.2 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196825 28217 0 None None None Human 4.2 pKi = 4.2 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11290688 28187 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 2 2 2.8 CN[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196599 28187 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 2 2 2.8 CN[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
16007117 161496 0 None -72 6 Human 7.1 pKi = 7.1 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 161496 0 None -72 6 Human 7.1 pKi = 7.1 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44582676 372889 0 None -57 17 Human 5.1 pKi = 5.1 Binding
Inhibition of human cloned dopamine D5 receptor by competitive binding experimentInhibition of human cloned dopamine D5 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 372889 0 None -57 17 Human 5.1 pKi = 5.1 Binding
Inhibition of human cloned dopamine D5 receptor by competitive binding experimentInhibition of human cloned dopamine D5 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44582675 365962 0 None -125 15 Human 5.1 pKi = 5.1 Binding
Inhibition of human cloned dopamine D5 receptor by competitive binding experimentInhibition of human cloned dopamine D5 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 365962 0 None -125 15 Human 5.1 pKi = 5.1 Binding
Inhibition of human cloned dopamine D5 receptor by competitive binding experimentInhibition of human cloned dopamine D5 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
145980271 331309 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 331309 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
17756212 177246 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 177246 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
42626289 294770 0 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
CHEMBL393492 294770 0 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
11442138 141450 0 None -1862 3 Rat 5.1 pKi = 5.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL192650 141450 0 None -1862 3 Rat 5.1 pKi = 5.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
11415988 28211 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N(C)C)C2 10.1021/jm040889k
CHEMBL1196757 28211 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N(C)C)C2 10.1021/jm040889k
137651322 313375 0 None -8709 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 313375 0 None -8709 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
11405458 27034 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 2 1 2 3.2 CN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1187931 27034 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 2 1 2 3.2 CN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
154706461 350317 1 None -331 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 350317 1 None -331 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
135398737 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
2818 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL253391 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 1973 61 None -83 61 Human 6.1 pKi = 6.1 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
154706431 350548 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 350548 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
11637457 145296 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 145296 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
11154555 1656 51 None -724 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 1656 51 None -724 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 1656 51 None -724 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 1656 51 None -724 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 1656 51 None -724 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
9801858 126154 0 None -12 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL179757 126154 0 None -12 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
14202 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
3036864 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
3082393 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
5018 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
6603800 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
71451380 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
943 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
956 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
CHEMBL13668 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
CHEMBL2158641 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
CHEMBL62 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
CHEMBL63321 4235 21 None -2 12 Human 8.1 pKi = 8.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 10.1021/jm040889k
46231646 447603 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL598515 447603 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
42625354 182405 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 349 6 0 3 3.2 O=C1c2ccccc2CN1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL240774 182405 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 349 6 0 3 3.2 O=C1c2ccccc2CN1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
44436308 182558 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.3 O=C1c2ccccc2CN1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL240996 182558 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.3 O=C1c2ccccc2CN1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
154705038 350608 1 None -245 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 350608 1 None -245 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
130442480 349282 0 None 1 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 349282 0 None 1 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
156011458 351256 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4636741 351256 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
11290269 28010 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 243 1 2 2 2.5 N[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1195331 28010 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 243 1 2 2 2.5 N[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11153135 27082 0 None None None Human 4.1 pKi = 4.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 341 7 0 2 5.0 CCCN(CCC)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188308 27082 0 None None None Human 4.1 pKi = 4.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 341 7 0 2 5.0 CCCN(CCC)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
71062708 310363 0 None -48 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 310363 0 None -48 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
57398351 142404 0 None -91 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 142404 0 None -91 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
154725001 350609 1 None -562 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 350609 1 None -562 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
154724650 350306 1 None -501 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 350306 1 None -501 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
11439190 462579 0 None -31 4 Human 7.1 pKi = 7.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 462579 0 None -31 4 Human 7.1 pKi = 7.1 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11631304 145584 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
CHEMBL201432 145584 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
11976 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
623 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
667466 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
667467 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
CHEMBL908 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
DB01239 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
440229 178378 35 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1021/acs.jmedchem.4c00537
CHEMBL2334891 178378 35 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to D5 receptor (unknown origin) assessed as inhibition constantBinding affinity to D5 receptor (unknown origin) assessed as inhibition constant
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1021/acs.jmedchem.4c00537
440229 178378 35 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 178378 35 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
17755867 176992 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 176992 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
135398745 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
1982 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
4585 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 5933 69 None -17 45 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
11221294 27045 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1187988 27045 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
182600 237540 2 None -10 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
CHEMBL341774 237540 2 None -10 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
56589561 142844 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 142844 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
16090821 163261 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 163261 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
135986088 352037 0 None -275 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
CHEMBL464811 352037 0 None -275 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
154727713 350333 1 None -10 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 350333 1 None -10 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154725277 350400 1 None -363 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 350400 1 None -363 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
137645574 313690 0 None -9999 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 313690 0 None -9999 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11698643 7376 16 None -181 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
6125 7376 16 None -181 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
CHEMBL209497 7376 16 None -181 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
17755868 289897 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 289897 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44396235 333211 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 333211 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
145968810 329948 0 None -33 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 329948 0 None -33 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
11450584 27065 0 None None None Human 5.0 pKi = 5.0 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 2 2 2.8 CN[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188142 27065 0 None None None Human 5.0 pKi = 5.0 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 2 2 2.8 CN[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11151473 28174 0 None None None Human 5.0 pKi = 5.0 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 243 1 2 2 2.5 N[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196485 28174 0 None None None Human 5.0 pKi = 5.0 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 243 1 2 2 2.5 N[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
76328715 216047 0 None -1047 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 216047 0 None -1047 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
49783209 41478 0 None -1698 27 Human 6.0 pKi = 6.0 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 41478 0 None -1698 27 Human 6.0 pKi = 6.0 Binding
Binding affinity to human dopamine D5 receptorBinding affinity to human dopamine D5 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
76328715 216047 0 None -1047 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 216047 0 None -1047 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
52936725 124010 25 None -39810 13 Human 6.0 pKi = 6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.6019/CHEMBL5442175
CHEMBL1766103 124010 25 None -39810 13 Human 6.0 pKi = 6 Binding
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.6019/CHEMBL5442175
5018 8054 7 None -1 2 Human 9.2 pKd = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 8051291
946 8054 7 None -1 2 Human 9.2 pKd = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 8051291
CHEMBL13668 8054 7 None -1 2 Human 9.2 pKd = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 8051291
2402 6855 40 None -79 14 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 6855 40 None -79 14 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 6855 40 None -79 14 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 6855 40 None -79 14 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 6855 40 None -79 14 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
11154555 1656 51 None -724 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 1656 51 None -724 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 1656 51 None -724 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 1656 51 None -724 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 1656 51 None -724 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
2470 7422 0 None -74 33 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 7422 0 None -74 33 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 7422 0 None -74 33 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 7422 0 None -74 33 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
104870 199119 37 None -1 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
2558 199119 37 None -1 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 199119 37 None -1 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 199119 37 None -1 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
1524 4448 0 None -34 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 4448 0 None -34 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 4448 0 None -34 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 4448 0 None -34 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 4448 0 None -34 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
100 8289 46 None -58 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 8289 46 None -58 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 8289 46 None -58 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 8289 46 None -58 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 8289 46 None -58 34 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 971 74 None -112 38 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 971 74 None -112 38 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 971 74 None -112 38 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 971 74 None -112 38 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 971 74 None -112 38 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2337 6622 53 None -1 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 6622 53 None -1 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 6622 53 None -1 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 6622 53 None -1 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 6622 53 None -1 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2407 6859 55 None -83 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 6859 55 None -83 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 6859 55 None -83 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 6859 55 None -83 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 6859 55 None -83 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
31101 1504 27 None -19 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 1504 27 None -19 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 1504 27 None -19 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 1504 27 None -19 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 1504 27 None -19 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1634 163834 36 None -20 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
4011 163834 36 None -20 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 163834 36 None -20 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
DB00934 163834 36 None -20 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
2150 139247 20 None -4 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
7077 139247 20 None -4 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 139247 20 None -4 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
DB11160 139247 20 None -4 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
154 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1621 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
638252 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 4804 8 None -25 23 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D5Binding affinity towards Dopamine receptor D5
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3294 4099 60 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 4099 60 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 4099 60 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 4099 60 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 4099 60 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
212 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
135398737 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2818 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL253391 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 1973 61 None -83 61 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
103 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 8980 49 None -3 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2105 6217 26 None -34 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 6217 26 None -34 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 6217 26 None -34 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 6217 26 None -34 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 6217 26 None -34 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
180 829 44 None -25 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 829 44 None -25 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 829 44 None -25 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 829 44 None -25 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 829 44 None -25 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2865 8961 54 None -12 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 8961 54 None -12 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 8961 54 None -12 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 8961 54 None -12 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 8961 54 None -12 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2080 352858 63 None 1 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
33630 352858 63 None 1 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 352858 63 None 1 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
DB13791 352858 63 None 1 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2726 1895 54 None -26 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 1895 54 None -26 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 1895 54 None -26 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 1895 54 None -26 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 1895 54 None -26 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1153 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 3349 35 None -14 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2389 6775 83 None -229 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 6775 83 None -229 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 6775 83 None -229 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 6775 83 None -229 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 6775 83 None -229 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135398745 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1982 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4585 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 5933 69 None -17 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1613 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1353 3909 69 None -42 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 3909 69 None -42 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 3909 69 None -42 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 3909 69 None -42 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 3909 69 None -42 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
115237 118408 70 None -5 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4137 118408 70 None -5 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 118408 70 None -5 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 118408 70 None -5 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
37 1606 47 None -9 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 1606 47 None -9 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 1606 47 None -9 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 1606 47 None -9 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 1606 47 None -9 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
228 919 20 None -6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 919 20 None -6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 919 20 None -6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 919 20 None -6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 919 20 None -6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
1212 3415 38 None -7 41 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 3415 38 None -7 41 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 3415 38 None -7 41 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 3415 38 None -7 41 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 3415 38 None -7 41 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1214 506896 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)C(F)(F)F None
3372 506896 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)C(F)(F)F None
11976 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
623 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667466 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 1897 43 None -2 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1211 477456 10 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 None
CHEMBL4743867 477456 10 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 None
1588 4738 26 None -19 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 4738 26 None -19 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 4738 26 None -19 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 4738 26 None -19 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 4738 26 None -19 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
681 3019 53 None -67 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 3019 53 None -67 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 3019 53 None -67 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 3019 53 None -67 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 3019 53 None -67 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
940 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
947 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
CHEMBL59 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
DB00988 3019 53 None -67 20 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
1242 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
6603799 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
6852376 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
935 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL24077 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL284746 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL286080 7344 19 None 1 6 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
6917970 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 25231919
8370 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 25231919
CHEMBL487387 7498 42 None 1 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 25231919
107930 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
14787976 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
3304 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
CHEMBL298406 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
CHEMBL56666 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
DB12273 3147 31 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 1826762
14202 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
3036864 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
3082393 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
5018 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
6603800 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
71451380 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
943 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
956 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
CHEMBL13668 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
CHEMBL2158641 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
CHEMBL62 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
CHEMBL63321 4235 21 None -2 12 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)Cl 1826762
10088113 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
1243 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
6604885 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
944 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
CHEMBL1473849 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
CHEMBL324017 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
CHEMBL416401 7354 32 None -2 13 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
1043 3255 6 None -15 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
149 3255 6 None -15 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
8223 3255 6 None -15 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL442 3255 6 None -15 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00696 3255 6 None -15 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
2601 8241 23 None -4 19 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 8241 23 None -4 19 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 8241 23 None -4 19 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 8241 23 None -4 19 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 8241 23 None -4 19 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
11954293 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3036780 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
4115 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 212936 14 None -5 28 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
484 5824 40 None -12 4 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
951 5824 40 None -12 4 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
CHEMBL432 5824 40 None -12 4 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
2470 7422 0 None -74 33 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
5265 7422 0 None -74 33 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
99 7422 0 None -74 33 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
CHEMBL267930 7422 0 None -74 33 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
5 285 48 None -3235 29 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
5202 285 48 None -3235 29 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
CHEMBL39 285 48 None -3235 29 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
DB08839 285 48 None -3235 29 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
1524 4448 0 None -34 27 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
3822 4448 0 None -34 27 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
88 4448 0 None -34 27 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
CHEMBL51 4448 0 None -34 27 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
DB12465 4448 0 None -34 27 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
100 8289 46 None -58 34 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
2637 8289 46 None -58 34 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
5452 8289 46 None -58 34 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
CHEMBL479 8289 46 None -58 34 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
DB00679 8289 46 None -58 34 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
30137 5860 0 None -31 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
8594 5860 0 None -31 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
934 5860 0 None -31 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
3153 611 19 None -15 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
932 611 19 None -15 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
CHEMBL26736 611 19 None -15 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
2407 6859 55 None -83 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
59227 6859 55 None -83 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
941 6859 55 None -83 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
CHEMBL1303 6859 55 None -83 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
DB05271 6859 55 None -83 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
1153 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 3349 35 None -14 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
31101 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
31101 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
35 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
403 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
CHEMBL493 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
DB01200 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 1504 27 None -19 28 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
1353 3909 69 None -42 49 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
3559 3909 69 None -42 49 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
86 3909 69 None -42 49 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
CHEMBL54 3909 69 None -42 49 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
DB00502 3909 69 None -42 49 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
937 7348 0 None 1 2 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1826762
135398737 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
2818 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
38 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
722 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
CHEMBL253391 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
CHEMBL42 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
DB00363 1973 61 None -83 61 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
2105 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2105 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
47811 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
48 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
CHEMBL531 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
DB01186 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 6217 26 None -34 25 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
161309 1266 0 None None None Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC[C@@H]([C@@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 1826762
988 1266 0 None None None Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC[C@@H]([C@@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 1826762
2726 1895 54 None -26 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
621 1895 54 None -26 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
83 1895 54 None -26 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
CHEMBL71 1895 54 None -26 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
DB00477 1895 54 None -26 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
228 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
228 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
33 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
6005 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
CHEMBL53 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
DB00714 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 919 20 None -6 24 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
37459 1538 8 None -47 10 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
62 1538 8 None -47 10 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
CHEMBL8514 1538 8 None -47 10 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
37 1606 47 None -9 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 1606 47 None -9 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 1606 47 None -9 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 1606 47 None -9 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 1606 47 None -9 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
1153 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 3349 35 None -14 8 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
1212 3415 38 None -7 41 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
204 3415 38 None -7 41 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
3372 3415 38 None -7 41 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL726 3415 38 None -7 41 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00623 3415 38 None -7 41 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
5281881 3411 13 None -7 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
948 3411 13 None -7 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL54661 3411 13 None -7 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00875 3411 13 None -7 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
1588 4738 26 None -19 28 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 4738 26 None -19 28 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 4738 26 None -19 28 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 4738 26 None -19 28 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 4738 26 None -19 28 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666