Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

10456166 119697 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL346692 119697 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL4285942 119697 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
52937876 61194 None 0 Human Functional pEC50 = 10.3 10.3 489 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 61194 None 0 Human Functional pEC50 = 10.3 10.3 489 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
24866114 178793 None 0 Human Functional pEC50 = 10.2 10.2 223 2
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL468017 178793 None 0 Human Functional pEC50 = 10.2 10.2 223 2
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
24754400 154690 None 0 Human Functional pEC50 = 10.1 10.1 19 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL399164 154690 None 0 Human Functional pEC50 = 10.1 10.1 19 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
24936081 178742 None 0 Human Functional pEC50 = 10.1 10.1 234 2
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL467540 178742 None 0 Human Functional pEC50 = 10.1 10.1 234 2
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
24866612 189730 None 0 Human Functional pEC50 = 10.1 10.1 72 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL514885 189730 None 0 Human Functional pEC50 = 10.1 10.1 72 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
2 3261 None 19 Human Functional pEC50 = 10.0 10.0 2 7
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
54562 3261 None 19 Human Functional pEC50 = 10.0 10.0 2 7
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
CHEMBL240773 3261 None 19 Human Functional pEC50 = 10.0 10.0 2 7
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
56941366 105755 None 0 Human Functional pEC50 = 10 10.0 158 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
CHEMBL3125990 105755 None 0 Human Functional pEC50 = 10 10.0 158 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
681 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
681.0 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
940 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
947 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
CHEMBL59 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
DB00988 1465 None 47 Human Functional pEC50 = 10.0 10.0 -2 15
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
24742011 94367 None 0 Human Functional pEC50 = 9.9 9.9 18 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL250552 94367 None 0 Human Functional pEC50 = 9.9 9.9 18 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
128 149 None 8 Human Functional pEC50 = 9.9 9.9 9 3
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
172267 149 None 8 Human Functional pEC50 = 9.9 9.9 9 3
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
CHEMBL273273 149 None 8 Human Functional pEC50 = 9.9 9.9 9 3
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
119570 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
119570.0 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3159 None 58 Rat Functional pEC50 = 9.7 9.7 2 11
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
17449900 139629 None 9 Human Functional pEC50 = 9.7 9.7 1 3
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139629 None 9 Human Functional pEC50 = 9.7 9.7 1 3
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
52941006 17106 None 0 Human Functional pEC50 = 9.6 9.6 208 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1254947 17106 None 0 Human Functional pEC50 = 9.6 9.6 208 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
60148494 80891 None 0 Human Functional pEC50 = 9.6 9.6 446 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152747 80891 None 0 Human Functional pEC50 = 9.6 9.6 446 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
60165801 80890 None 0 Human Functional pEC50 = 9.6 9.6 446 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL2152746 80890 None 0 Human Functional pEC50 = 9.6 9.6 446 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
85470564 156915 None 0 Human Functional pEC50 = 9.5 9.5 37 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156915 None 0 Human Functional pEC50 = 9.5 9.5 37 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
137633863 156716 None 0 Human Functional pEC50 = 9.5 9.5 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156716 None 0 Human Functional pEC50 = 9.5 9.5 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137633863 156716 None 0 Human Functional pEC50 = 9.5 9.5 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156716 None 0 Human Functional pEC50 = 9.5 9.5 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
132578416 173910 None 0 Human Functional pEC50 = 9.5 9.5 -1 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4538230 173910 None 0 Human Functional pEC50 = 9.5 9.5 -1 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
25256816 181714 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 181714 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
5311346 206612 None 20 Rat Functional pEC50 = 9.4 9.4 467 5
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 206612 None 20 Rat Functional pEC50 = 9.4 9.4 467 5
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 206612 None 20 Rat Functional pEC50 = 9.4 9.4 467 5
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
9888555 165699 None 19 Human Functional pEC50 = 9.4 9.4 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 165699 None 19 Human Functional pEC50 = 9.4 9.4 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
2 3261 None 19 Human Functional pEC50 = 9.4 9.4 2 7
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
54562 3261 None 19 Human Functional pEC50 = 9.4 9.4 2 7
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
CHEMBL240773 3261 None 19 Human Functional pEC50 = 9.4 9.4 2 7
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
137651936 157484 None 0 Human Functional pEC50 = 9.4 9.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 9.4 9.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137651936 157484 None 0 Human Functional pEC50 = 9.4 9.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 9.4 9.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 159173 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 159173 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
45486325 200876 None 0 Human Functional pEC50 = 9.3 9.3 158 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2ccnc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL577073 200876 None 0 Human Functional pEC50 = 9.3 9.3 158 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2ccnc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
45486330 200248 None 0 Human Functional pEC50 = 9.3 9.3 173 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL571992 200248 None 0 Human Functional pEC50 = 9.3 9.3 173 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
45486328 199818 None 0 Human Functional pEC50 = 9.3 9.3 25 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL569107 199818 None 0 Human Functional pEC50 = 9.3 9.3 25 2
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
71459659 83869 None 0 Human Functional pEC50 = 9.3 9.3 3 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206264 83869 None 0 Human Functional pEC50 = 9.3 9.3 3 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11957566 184 None 17 Human Functional pEC50 = 9.3 9.3 1 4
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
1219 184 None 17 Human Functional pEC50 = 9.3 9.3 1 4
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
3296 184 None 17 Human Functional pEC50 = 9.3 9.3 1 4
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
950 184 None 17 Human Functional pEC50 = 9.3 9.3 1 4
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
CHEMBL285755 184 None 17 Human Functional pEC50 = 9.3 9.3 1 4
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
60148495 80899 None 0 Human Functional pEC50 = 9.3 9.3 125 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152755 80899 None 0 Human Functional pEC50 = 9.3 9.3 125 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
11299620 97337 None 1 Human Functional pEC50 = 9.2 9.2 64 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL269004 97337 None 1 Human Functional pEC50 = 9.2 9.2 64 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
681 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
681.0 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
940 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
947 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
CHEMBL59 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
DB00988 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
681 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
681.0 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
940 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
947 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
CHEMBL59 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
DB00988 1465 None 47 Human Functional pEC50 = 9.2 9.2 -2 15
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00417
10178704 49673 None 0 Human Functional pEC50 = 9.2 9.2 17 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
CHEMBL156639 49673 None 0 Human Functional pEC50 = 9.2 9.2 17 2
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
14465382 157074 None 1 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
CHEMBL4073068 157074 None 1 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
45140376 203114 None 0 Human Functional pEC50 = 9.1 9.1 2 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
CHEMBL599635 203114 None 0 Human Functional pEC50 = 9.1 9.1 2 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
155522454 170818 None 0 Human Functional pEC50 = 9.1 9.1 2 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4452046 170818 None 0 Human Functional pEC50 = 9.1 9.1 2 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
119570 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
119570.0 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3159 None 58 Human Functional pEC50 = 9.1 9.1 -2 11
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
45486330 200248 None 0 Human Functional pEC50 = 9.1 9.1 173 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL571992 200248 None 0 Human Functional pEC50 = 9.1 9.1 173 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
45486330 200248 None 0 Human Functional pEC50 = 9.1 9.1 173 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL571992 200248 None 0 Human Functional pEC50 = 9.1 9.1 173 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
127038171 137010 None 0 Human Functional pEC50 = 9.1 9.1 46 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742140 137010 None 0 Human Functional pEC50 = 9.1 9.1 46 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742430 137010 None 0 Human Functional pEC50 = 9.1 9.1 46 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
137460109 191492 None 0 Human Functional pEC50 = 9.1 9.1 -3 2
Agonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5192367 191492 None 0 Human Functional pEC50 = 9.1 9.1 -3 2
Agonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
60148496 80896 None 0 Human Functional pEC50 = 9.1 9.1 100 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2c[nH]c3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152752 80896 None 0 Human Functional pEC50 = 9.1 9.1 100 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2c[nH]c3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
681 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
681.0 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
940 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
947 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
CHEMBL59 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
DB00988 1465 None 47 Human Functional pEC50 = 9.1 9.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
85470564 156915 None 0 Human Functional pEC50 = 9.1 9.1 37 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156915 None 0 Human Functional pEC50 = 9.1 9.1 37 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466573 158628 None 0 Human Functional pEC50 = 9.1 9.1 16 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4091498 158628 None 0 Human Functional pEC50 = 9.1 9.1 16 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466716 161097 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099236 161097 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116199 161097 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
85469680 156807 None 0 Human Functional pEC50 = 9.0 9.0 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156807 None 0 Human Functional pEC50 = 9.0 9.0 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
71459660 83870 None 0 Human Functional pEC50 = 9.0 9.0 -2 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206265 83870 None 0 Human Functional pEC50 = 9.0 9.0 -2 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11957566 184 None 17 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
1219 184 None 17 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
3296 184 None 17 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
950 184 None 17 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
CHEMBL285755 184 None 17 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
44427827 93328 None 0 Human Functional pEC50 = 9 9.0 15 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 93328 None 0 Human Functional pEC50 = 9 9.0 15 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
119570 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
119570.0 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
2233 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
953 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
CHEMBL301265 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
DB00413 3159 None 58 Human Functional pEC50 = 9 9.0 -2 11
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
57242 3259 None 18 Human Functional pEC50 = 9 9.0 9 4
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
954 3259 None 18 Human Functional pEC50 = 9 9.0 9 4
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
CHEMBL155731 3259 None 18 Human Functional pEC50 = 9 9.0 9 4
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
85469680 156807 None 0 Human Functional pEC50 = 9 9.0 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156807 None 0 Human Functional pEC50 = 9 9.0 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466574 158686 None 0 Human Functional pEC50 = 9 9.0 3 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158686 None 0 Human Functional pEC50 = 9 9.0 3 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466574 158686 None 0 Human Functional pEC50 = 9 9.0 3 2
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
CHEMBL4092052 158686 None 0 Human Functional pEC50 = 9 9.0 3 2
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
16038360 16976 None 0 Human Functional pEC50 = 9.0 9.0 104 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1253770 16976 None 0 Human Functional pEC50 = 9.0 9.0 104 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
10411237 117546 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL339960 117546 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL4287055 117546 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
137660062 159480 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 370 7 1 2 6.5 CCCCCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
CHEMBL4100634 159480 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 370 7 1 2 6.5 CCCCCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
10368423 97980 None 0 Green monkey Functional pEC50 = 8.9 8.9 - 1
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 493 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)cc2)CC1 10.1021/jm030836n
CHEMBL27254 97980 None 0 Green monkey Functional pEC50 = 8.9 8.9 - 1
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 493 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)cc2)CC1 10.1021/jm030836n
155531663 171772 None 0 Human Functional pEC50 = 8.9 8.9 7 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1cc(O)ccc1O)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4466245 171772 None 0 Human Functional pEC50 = 8.9 8.9 7 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1cc(O)ccc1O)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
45273211 198083 None 0 Human Functional pEC50 = 8.9 8.9 33 2
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
CHEMBL556269 198083 None 0 Human Functional pEC50 = 8.9 8.9 33 2
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
128 149 None 8 Human Functional pEC50 = 8.9 8.9 9 3
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
172267 149 None 8 Human Functional pEC50 = 8.9 8.9 9 3
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
CHEMBL273273 149 None 8 Human Functional pEC50 = 8.9 8.9 9 3
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
60148497 80883 None 0 Human Functional pEC50 = 8.9 8.9 2 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152633 80883 None 0 Human Functional pEC50 = 8.9 8.9 2 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
2 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
54562 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
90467024 157781 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157781 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
2 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.9 8.9 2 7
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
10476504 33495 None 1 Human Functional pEC50 = 8.9 8.9 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 33495 None 1 Human Functional pEC50 = 8.9 8.9 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
127037825 137006 None 0 Human Functional pEC50 = 8.9 8.9 2 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740041 137006 None 0 Human Functional pEC50 = 8.9 8.9 2 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742426 137006 None 0 Human Functional pEC50 = 8.9 8.9 2 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
24759792 184514 None 0 Human Functional pEC50 = 8.9 8.9 190 2
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL484598 184514 None 0 Human Functional pEC50 = 8.9 8.9 190 2
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
90467024 157781 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157781 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
60194424 80467 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 511 9 2 7 4.3 CCCN(CC[C@H]1CC[C@H](NS(=O)(=O)c2cccnc2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
CHEMBL2146499 80467 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 511 9 2 7 4.3 CCCN(CC[C@H]1CC[C@H](NS(=O)(=O)c2cccnc2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
119570 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
119570.0 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3159 None 58 Human Functional pEC50 = 8.8 8.8 -2 11
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
10092819 16780 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 16780 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
24866612 189730 None 0 Human Functional pEC50 = 8.8 8.8 72 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL514885 189730 None 0 Human Functional pEC50 = 8.8 8.8 72 2
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
53361666 190730 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5181007 190730 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
45140377 203115 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2c(O)cccc2C1 10.1021/jm901618d
CHEMBL599636 203115 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2c(O)cccc2C1 10.1021/jm901618d
169410194 196730 None 6 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
169410194 196730 None 6 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
681 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
681.0 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
940 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
947 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
DB00988 1465 None 47 Human Functional pEC50 = 8.8 8.8 -2 15
Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysisAgonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
171492446 196607 None 0 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
171492446 196607 None 0 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
137660417 159248 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 159248 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
53475319 83548 None 8 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrsAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs
ChEMBL 478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1 10.1021/ml200100t
CHEMBL2203406 83548 None 8 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrsAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs
ChEMBL 478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1 10.1021/ml200100t
2 3261 None 19 Rat Functional pEC50 = 8.8 8.8 -4 7
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
54562 3261 None 19 Rat Functional pEC50 = 8.8 8.8 -4 7
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
CHEMBL240773 3261 None 19 Rat Functional pEC50 = 8.8 8.8 -4 7
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
2 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
54562 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
2 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
54562 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.8 8.8 2 7
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
3038495 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
3038495 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 708 None 33 Human Functional pEC50 = 8.7 8.7 -8 8
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
11154555 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
5037 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
7671 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
25071384 111844 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111844 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
11154555 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
5037 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
7671 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.7 8.7 -1 10
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
25071384 111844 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111844 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
2 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.7 8.7 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 8 8.0 2 7
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
54562 3261 None 19 Human Functional pEC50 = 8 8.0 2 7
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8 8.0 2 7
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
16078 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
16078.0 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
2424 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
4109 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
CHEMBL465 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
DB00470 1362 None 15 Human Functional pEC50 = 8.0 8.0 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
2402 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
5095 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
5095.0 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
7295 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
CHEMBL589 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
DB00268 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
2402 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
5095 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
5095.0 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
7295 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
CHEMBL589 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
DB00268 3370 None 38 Human Functional pEC50 = 8.0 8.0 5 17
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
127047458 139822 None 0 Human Functional pEC50 = 8.0 8.0 1 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 419 7 1 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3798334 139822 None 0 Human Functional pEC50 = 8.0 8.0 1 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 419 7 1 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
681 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
681.0 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
940 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
947 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
DB00988 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
127037828 137009 None 0 Human Functional pEC50 = 8.0 8.0 30 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740778 137009 None 0 Human Functional pEC50 = 8.0 8.0 30 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742429 137009 None 0 Human Functional pEC50 = 8.0 8.0 30 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
77461254 191333 None 0 Human Functional pEC50 = 7 7.0 -1 2
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5189785 191333 None 0 Human Functional pEC50 = 7 7.0 -1 2
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
164609493 184542 None 0 Human Functional pEC50 = 7.0 7.0 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 184542 None 0 Human Functional pEC50 = 7.0 7.0 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
168292954 193106 None 0 Human Functional pEC50 = 6.0 6.0 -7 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 193106 None 0 Human Functional pEC50 = 6.0 6.0 -7 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 193106 None 0 Human Functional pEC50 = 6.0 6.0 -7 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168295541 193149 None 0 Human Functional pEC50 = 6.0 6.0 -14 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 193149 None 0 Human Functional pEC50 = 6.0 6.0 -14 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 193149 None 0 Human Functional pEC50 = 6.0 6.0 -14 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
90467323 159652 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 159652 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
122181332 121939 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121939 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
90467022 156010 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4060896 156010 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
127045794 140195 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3797771 140195 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800680 140195 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
127046015 140199 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
CHEMBL3799465 140199 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
CHEMBL3800684 140199 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
25072635 111846 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111846 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
90467323 159652 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 159652 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
11706497 78206 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 78206 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
25072635 111846 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111846 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
122181332 121939 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121939 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
164619170 185707 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164619170 185707 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
25071692 111852 None 0 Human Functional pEC50 = 7.9 7.9 9 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111852 None 0 Human Functional pEC50 = 7.9 7.9 9 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
90467322 156901 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156901 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
25071692 111852 None 0 Human Functional pEC50 = 7.9 7.9 9 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111852 None 0 Human Functional pEC50 = 7.9 7.9 9 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
155516042 176398 None 0 Human Functional pEC50 = 7.9 7.9 794 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 176398 None 0 Human Functional pEC50 = 7.9 7.9 794 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 176398 None 0 Human Functional pEC50 = 7.9 7.9 794 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
164628178 186453 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628178 186453 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
90467172 156987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4072140 156987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90467317 155881 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.1 O=C(NCCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4059573 155881 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.1 O=C(NCCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
168295528 193140 None 0 Human Functional pEC50 = 5.9 5.9 -56 9
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193140 None 0 Human Functional pEC50 = 5.9 5.9 -56 9
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193140 None 0 Human Functional pEC50 = 5.9 5.9 -56 9
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
172463952 196538 None 0 Human Functional pEC50 = 6.9 6.9 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 6.9 6.9 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172463952 196538 None 0 Human Functional pEC50 = 6.9 6.9 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 6.9 6.9 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
164628178 186453 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628178 186453 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9828632 100124 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL287198 100124 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
90467173 158290 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 443 8 1 4 5.4 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4087889 158290 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 443 8 1 4 5.4 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
164938010 195433 None 0 Human Functional pEC50 = 4.9 4.9 -117 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5403610 195433 None 0 Human Functional pEC50 = 4.9 4.9 -117 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
44443903 154167 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 219 3 1 3 2.0 C=CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL398480 154167 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 219 3 1 3 2.0 C=CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
168294449 193127 None 0 Human Functional pEC50 = 5.9 5.9 -50 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 193127 None 0 Human Functional pEC50 = 5.9 5.9 -50 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 193127 None 0 Human Functional pEC50 = 5.9 5.9 -50 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
85469680 156807 None 0 Human Functional pEC50 = 7.9 7.9 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156807 None 0 Human Functional pEC50 = 7.9 7.9 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466574 158686 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158686 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466425 159408 None 0 Human Functional pEC50 = 7.9 7.9 10 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 159408 None 0 Human Functional pEC50 = 7.9 7.9 10 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
90467319 161130 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4095588 161130 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116454 161130 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
127045797 140198 None 0 Human Functional pEC50 = 7.9 7.9 21 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
CHEMBL3798372 140198 None 0 Human Functional pEC50 = 7.9 7.9 21 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
CHEMBL3800683 140198 None 0 Human Functional pEC50 = 7.9 7.9 21 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
90466574 158686 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158686 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
127047310 140162 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 433 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800489 140162 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 433 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
145988474 167247 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 379 7 2 5 2.8 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(C#N)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4290759 167247 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 379 7 2 5 2.8 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(C#N)cc1)CC2 10.1021/acsmedchemlett.8b00229
154703875 176553 None 1 Human Functional pEC50 = 6.8 6.8 6 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 176553 None 1 Human Functional pEC50 = 6.8 6.8 6 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 176553 None 1 Human Functional pEC50 = 6.8 6.8 6 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
172463952 196538 None 0 Human Functional pEC50 = 5.8 5.8 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 5.8 5.8 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5077114 216970 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
172463952 196538 None 0 Human Functional pEC50 = 5.8 5.8 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 5.8 5.8 -20 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
136056636 111851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90467021 156762 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156762 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
136056636 111851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90467021 156762 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156762 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
164609729 185204 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 185204 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
171492372 197072 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
164612037 185483 None 0 Human Functional pEC50 = 7.8 7.8 6 11
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 185483 None 0 Human Functional pEC50 = 7.8 7.8 6 11
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
90466864 158762 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4092900 158762 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90467171 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
90467171 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 161242 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
11581443 96454 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1021/jm050729o
CHEMBL26188 96454 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1021/jm050729o
171492372 197072 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5089655 217710 None 0 Human Functional pEC50 = 6.8 6.8 63 2
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
164616851 185056 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 185056 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
137658100 159710 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4103339 159710 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
164937999 197010 None 0 Human Functional pEC50 = 7.8 7.8 6 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 6 0 5 3.8 c1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5436702 197010 None 0 Human Functional pEC50 = 7.8 7.8 6 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 6 0 5 3.8 c1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
44309775 102733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL304605 102733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
44309775 102733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/s0960-894x(03)00389-5
CHEMBL304605 102733 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/s0960-894x(03)00389-5
172444851 195152 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 474 10 0 2 6.4 CCCN(CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1)[C@@H]1C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00417
CHEMBL5397609 195152 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 474 10 0 2 6.4 CCCN(CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1)[C@@H]1C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00417
154705015 176619 None 1 Human Functional pEC50 = 6.8 6.8 91 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 176619 None 1 Human Functional pEC50 = 6.8 6.8 91 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 176619 None 1 Human Functional pEC50 = 6.8 6.8 91 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
25093832 155970 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155970 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
90467171 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
11678172 78061 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 78061 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
90467171 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4079093 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4117318 161242 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
25093832 155970 None 0 Human Functional pEC50 = 7.7 7.7 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155970 None 0 Human Functional pEC50 = 7.7 7.7 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
90467021 156762 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156762 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
25072941 156565 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
11510684 98707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
CHEMBL277301 98707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
2 3261 None 19 Human Functional pEC50 = 6.7 6.7 2 7
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
54562 3261 None 19 Human Functional pEC50 = 6.7 6.7 2 7
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.7 6.7 2 7
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
25072002 156205 None 0 Human Functional pEC50 = 7.7 7.7 3 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 7.7 7.7 3 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25072941 156565 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
90467024 157781 None 0 Human Functional pEC50 = 7.7 7.7 10 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157781 None 0 Human Functional pEC50 = 7.7 7.7 10 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
25072002 156205 None 0 Human Functional pEC50 = 7.7 7.7 3 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 7.7 7.7 3 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
127046755 140192 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3798943 140192 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800677 140192 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
2402 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
5095 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
5095.0 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
7295 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
CHEMBL589 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
DB00268 3370 None 38 Human Functional pEC50 = 7.7 7.7 5 17
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
172464337 196969 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172464337 196969 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
90466867 156402 None 0 Human Functional pEC50 = 7.7 7.7 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 156402 None 0 Human Functional pEC50 = 7.7 7.7 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
168281746 192991 None 0 Human Functional pEC50 = 5.7 5.7 -77 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192991 None 0 Human Functional pEC50 = 5.7 5.7 -77 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192991 None 0 Human Functional pEC50 = 5.7 5.7 -77 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
44436605 149151 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 149151 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
44400674 125256 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 125256 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
681 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
681.0 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
940 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
947 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
DB00988 1465 None 47 Human Functional pEC50 = 8.7 8.7 -2 15
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
44436600 91836 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 91836 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
90466571 159491 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 458 8 2 5 3.8 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4100735 159491 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 458 8 2 5 3.8 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
25139181 184448 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 184448 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
11316847 70371 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
CHEMBL194493 70371 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
15389743 184515 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.03.015
CHEMBL484599 184515 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.03.015
24805287 184880 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 2 0 4 2.5 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)COC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL485128 184880 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 2 0 4 2.5 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)COC4=O 10.1016/j.bmcl.2009.03.015
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayAgonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.3c00417
90466425 159408 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 159408 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
54580906 61625 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 61625 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
90466425 159408 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 159408 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
122181330 121937 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121937 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
90466717 157002 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 157002 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
2 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
54562 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.6 8.6 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
155525527 171171 None 0 Human Functional pEC50 = 8.6 8.6 8 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4457171 171171 None 0 Human Functional pEC50 = 8.6 8.6 8 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
90466717 157002 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 157002 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
3038495 708 None 33 Human Functional pEC50 = 8.6 8.6 -8 8
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 708 None 33 Human Functional pEC50 = 8.6 8.6 -8 8
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 708 None 33 Human Functional pEC50 = 8.6 8.6 -8 8
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
1353 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
3559 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
3559.0 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
86 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
CHEMBL54 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
DB00502 1911 None 63 Human Functional pEC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
46893146 61627 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 61627 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10084583 104834 None 3 Human Functional pEC50 = 8.6 8.6 9 3
Effective concentration required for agonistic activity against human Dopamine receptor D3Effective concentration required for agonistic activity against human Dopamine receptor D3
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104834 None 3 Human Functional pEC50 = 8.6 8.6 9 3
Effective concentration required for agonistic activity against human Dopamine receptor D3Effective concentration required for agonistic activity against human Dopamine receptor D3
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
172444647 195417 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
172444647 195417 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
44588497 175739 None 0 Human Functional pEC50 = 8.5 8.5 3 2
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)[C@H]1CCc2ccc(O)cc2C1 10.1016/j.ejmech.2022.114378
CHEMBL458088 175739 None 0 Human Functional pEC50 = 8.5 8.5 3 2
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)[C@H]1CCc2ccc(O)cc2C1 10.1016/j.ejmech.2022.114378
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -6 33
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
90466867 156402 None 0 Human Functional pEC50 = 7.7 7.7 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 156402 None 0 Human Functional pEC50 = 7.7 7.7 5 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
44438230 93610 None 2 Human Functional pEC50 = 7.7 7.7 -9 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 93610 None 2 Human Functional pEC50 = 7.7 7.7 -9 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
155563589 175422 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4573578 175422 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
127046238 139774 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)OC1CCCc2ccccc21 10.1039/C5MD00590F
CHEMBL3798010 139774 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)OC1CCCc2ccccc21 10.1039/C5MD00590F
172450959 195711 None 0 Human Functional pEC50 = 6.7 6.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 6.7 6.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
172450959 195711 None 0 Human Functional pEC50 = 5.7 5.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 5.7 5.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
11596603 9936 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm050729o
CHEMBL114541 9936 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm050729o
172450959 195711 None 0 Human Functional pEC50 = 6.7 6.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 6.7 6.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
172450959 195711 None 0 Human Functional pEC50 = 5.7 5.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 5.7 5.7 -162 4
Partial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D3 receptor (unknown origin) expressed in HEK293T co-expressing G-alpha oA assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
127046753 140191 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3799147 140191 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800675 140191 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
137660417 159248 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 159248 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
42625290 56262 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL1627316 56262 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
137660417 159248 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 159248 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
164622330 185968 None 0 Human Functional pEC50 = 6.6 6.6 11 2
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185968 None 0 Human Functional pEC50 = 6.6 6.6 11 2
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
162665657 182482 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 427 7 1 4 4.8 O=C(NC/C=C/CN1CCN(c2ccccc2)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4785109 182482 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 427 7 1 4 4.8 O=C(NC/C=C/CN1CCN(c2ccccc2)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
164614549 185049 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 185049 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
90467322 156901 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156901 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
44438197 153361 None 1 Human Functional pEC50 = 6.6 6.6 -6 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 153361 None 1 Human Functional pEC50 = 6.6 6.6 -6 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
56852956 112106 None 1 Human Functional pEC50 = 5.6 5.6 -281 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL3289656 112106 None 1 Human Functional pEC50 = 5.6 5.6 -281 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
90467322 156901 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156901 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
11307083 63576 None 0 Human Functional pEC50 = 7.6 7.6 6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
CHEMBL180060 63576 None 0 Human Functional pEC50 = 7.6 7.6 6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
90467170 161248 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4063681 161248 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4117347 161248 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
44438228 93609 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 93609 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
2 3261 None 19 Human Functional pEC50 = 7.6 7.6 2 7
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
54562 3261 None 19 Human Functional pEC50 = 7.6 7.6 2 7
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.6 7.6 2 7
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
164916968 196909 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
CHEMBL5434650 196909 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
127045793 140194 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3798841 140194 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800679 140194 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
164916968 196909 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
CHEMBL5434650 196909 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
CHEMBL5073754 216793 None 0 Human Functional pEC50 = 7.6 7.6 41 2
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
137659303 159398 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 159398 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
164608815 184560 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 184560 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
168475887 195235 None 2 Human Functional pEC50 = 6.6 6.6 10 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
CHEMBL5399270 195235 None 2 Human Functional pEC50 = 6.6 6.6 10 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
137659303 159398 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 159398 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
15006491 4562 None 3 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL102463 4562 None 3 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
168475888 196855 None 2 Human Functional pEC50 = 6.6 6.6 -1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 410 6 1 3 5.6 Clc1ccc([C@@H]2C[C@H]2NCCC2(c3ccccn3)CCOC3(CCCC3)C2)cc1 10.1021/acs.jmedchem.3c00417
CHEMBL5433458 196855 None 2 Human Functional pEC50 = 6.6 6.6 -1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 410 6 1 3 5.6 Clc1ccc([C@@H]2C[C@H]2NCCC2(c3ccccn3)CCOC3(CCCC3)C2)cc1 10.1021/acs.jmedchem.3c00417
15232477 169534 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL442535 169534 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
25072633 159314 None 0 Human Functional pEC50 = 7.5 7.5 -7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 7.5 7.5 -7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
164611757 185009 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 185009 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
168294767 193128 None 0 Human Functional pEC50 = 5.6 5.6 -87 10
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193128 None 0 Human Functional pEC50 = 5.6 5.6 -87 10
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193128 None 0 Human Functional pEC50 = 5.6 5.6 -87 10
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
25072633 159314 None 0 Human Functional pEC50 = 7.5 7.5 -7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 7.5 7.5 -7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
154726381 176632 None 1 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 176632 None 1 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 176632 None 1 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
168273640 192914 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192914 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192914 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164916968 196909 None 0 Human Functional pEC50 = 5.5 5.5 12 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
CHEMBL5434650 196909 None 0 Human Functional pEC50 = 5.5 5.5 12 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
3038495 708 None 33 Green monkey Functional pEC50 = 8.5 8.5 -5 8
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
7625 708 None 33 Green monkey Functional pEC50 = 8.5 8.5 -5 8
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
CHEMBL25236 708 None 33 Green monkey Functional pEC50 = 8.5 8.5 -5 8
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
3038495 708 None 33 Human Functional pEC50 = 8.5 8.5 -8 8
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 708 None 33 Human Functional pEC50 = 8.5 8.5 -8 8
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 708 None 33 Human Functional pEC50 = 8.5 8.5 -8 8
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
25139479 184423 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 184423 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
54580905 61623 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 61623 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
25256814 181718 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 181718 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
11983282 139030 None 0 Human Functional pEC50 = 8.5 8.5 2 3
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 139030 None 0 Human Functional pEC50 = 8.5 8.5 2 3
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
44427836 144048 None 0 Human Functional pEC50 = 8.5 8.5 20 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL390253 144048 None 0 Human Functional pEC50 = 8.5 8.5 20 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 2 7
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
76329028 105752 None 0 Human Functional pEC50 = 8.5 8.5 10 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 9 1 7 4.8 CCCN(CCN1CCN(c2ccc(-c3cccc(OC)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
CHEMBL3125987 105752 None 0 Human Functional pEC50 = 8.5 8.5 10 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 9 1 7 4.8 CCCN(CCN1CCN(c2ccc(-c3cccc(OC)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
681 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
681.0 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
940 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
947 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
DB00988 1465 None 47 Human Functional pEC50 = 8.5 8.5 -2 15
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
44436608 146844 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 146844 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
44400626 70426 None 0 Human Functional pEC50 = 8.5 8.5 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70426 None 0 Human Functional pEC50 = 8.5 8.5 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
154726792 176689 None 1 Human Functional pEC50 = 8.5 8.5 676 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 176689 None 1 Human Functional pEC50 = 8.5 8.5 676 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 176689 None 1 Human Functional pEC50 = 8.5 8.5 676 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
90467168 158544 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4090581 158544 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90467168 158544 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
CHEMBL4090581 158544 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
137634366 156135 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4062484 156135 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
137640863 157146 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4073966 157146 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 9 2 5 4.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
137633705 156709 None 0 Human Functional pEC50 = 8.4 8.4 158 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 156709 None 0 Human Functional pEC50 = 8.4 8.4 158 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
11761412 117015 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr-negative cells assessed as stimulation of [3H]-thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in CHO dhfr-negative cells assessed as stimulation of [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 117015 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr-negative cells assessed as stimulation of [3H]-thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in CHO dhfr-negative cells assessed as stimulation of [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
44427835 92218 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 540 9 1 6 4.9 CC(=O)OC(CCNC(=O)c1ccc(-c2ccccn2)cc1)CN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm0704200
CHEMBL242434 92218 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 540 9 1 6 4.9 CC(=O)OC(CCNC(=O)c1ccc(-c2ccccn2)cc1)CN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm0704200
90467323 159652 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 159652 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
44400585 68677 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68677 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
127037826 137007 None 0 Human Functional pEC50 = 8.4 8.4 8 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740286 137007 None 0 Human Functional pEC50 = 8.4 8.4 8 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742427 137007 None 0 Human Functional pEC50 = 8.4 8.4 8 2
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
71660285 90650 None 0 Human Functional pEC50 = 7.5 7.5 5 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 392 7 1 4 3.7 CCCN(CCN1CCN(c2ccccc2)CC1)[C@@H]1CCc2ccc(N)cc2C1 10.1016/j.bmc.2013.03.059
CHEMBL2387709 90650 None 0 Human Functional pEC50 = 7.5 7.5 5 2
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 392 7 1 4 3.7 CCCN(CCN1CCN(c2ccccc2)CC1)[C@@H]1CCc2ccc(N)cc2C1 10.1016/j.bmc.2013.03.059
137651073 157560 None 0 Human Functional pEC50 = 7.5 7.5 36 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 157560 None 0 Human Functional pEC50 = 7.5 7.5 36 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
164610892 185304 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 185304 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
137651073 157560 None 0 Human Functional pEC50 = 7.5 7.5 36 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 157560 None 0 Human Functional pEC50 = 7.5 7.5 36 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
44309510 102177 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 531 7 1 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1016/s0960-894x(03)00389-5
CHEMBL302374 102177 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 531 7 1 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1016/s0960-894x(03)00389-5
172449716 195885 None 0 Human Functional pEC50 = 6.5 6.5 8 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 682 13 1 6 5.0 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5412606 195885 None 0 Human Functional pEC50 = 6.5 6.5 8 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 682 13 1 6 5.0 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
10466682 94289 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 237 3 2 4 1.9 CCCN1CCO[C@H](c2cc(O)cc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL250003 94289 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 237 3 2 4 1.9 CCCN1CCO[C@H](c2cc(O)cc(O)c2)C1 10.1016/j.bmcl.2007.10.059
71452040 1091 None 1 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
9190 1091 None 1 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
CHEMBL2180638 1091 None 1 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
90466716 161097 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099236 161097 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116199 161097 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
164611342 185194 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 185194 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
90467321 161209 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 459 9 1 5 5.1 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4068218 161209 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 459 9 1 5 5.1 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4117124 161209 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 459 9 1 5 5.1 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
137634366 156135 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4062484 156135 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
137634366 156135 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4062484 156135 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1 10.1021/acs.jmedchem.6b01578
44438218 93502 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246020 93502 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44443923 155051 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 239 3 1 3 2.3 CCCN1CCOC(c2ccc(F)c(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL401157 155051 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 239 3 1 3 2.3 CCCN1CCOC(c2ccc(F)c(O)c2)C1 10.1016/j.bmcl.2007.10.059
10014484 94288 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 239 3 1 3 2.3 CCCN1CCO[C@H](c2ccc(F)c(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL250002 94288 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 239 3 1 3 2.3 CCCN1CCO[C@H](c2ccc(F)c(O)c2)C1 10.1016/j.bmcl.2007.10.059
10515841 210724 None 0 Rat Functional pEC50 = 7.4 7.4 3 2
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
CHEMBL98836 210724 None 0 Rat Functional pEC50 = 7.4 7.4 3 2
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
145989012 167402 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
CHEMBL4293886 167402 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
137636351 155963 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 155963 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
44443930 154820 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 237 3 2 4 1.9 CCCN1CCOC(c2cc(O)cc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL399892 154820 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 237 3 2 4 1.9 CCCN1CCOC(c2cc(O)cc(O)c2)C1 10.1016/j.bmcl.2007.10.059
90467452 158532 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4090459 158532 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
164619127 185631 None 0 Human Functional pEC50 = 7.4 7.4 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.4 7.4 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164619127 185631 None 0 Human Functional pEC50 = 7.4 7.4 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.4 7.4 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
127045792 140193 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 489 7 1 4 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(F)c2ccccc12 10.1039/C5MD00590F
CHEMBL3799311 140193 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 489 7 1 4 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(F)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800678 140193 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 489 7 1 4 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(F)c2ccccc12 10.1039/C5MD00590F
90466867 156402 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 156402 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466867 156402 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
CHEMBL4065510 156402 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
90467172 156987 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4072140 156987 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90467172 156987 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4072140 156987 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
172439985 195264 None 0 Human Functional pEC50 = 5.4 5.4 -35 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5399720 195264 None 0 Human Functional pEC50 = 5.4 5.4 -35 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
137655735 159084 None 0 Human Functional pEC50 = 7.4 7.4 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 159084 None 0 Human Functional pEC50 = 7.4 7.4 12 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25071691 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
90466864 158762 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4092900 158762 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90466864 158762 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4092900 158762 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
164916930 195492 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 680 13 2 7 4.0 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5404724 195492 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 680 13 2 7 4.0 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
25071691 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
60165418 75375 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL2037521 75375 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
168278471 192957 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192957 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192957 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
681 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
681.0 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
940 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
947 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
DB00988 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assayAgonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00976
2402 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
5095 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
5095.0 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
7295 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
CHEMBL589 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
DB00268 3370 None 38 Human Functional pEC50 = 8.4 8.4 5 17
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmcl.2007.10.059
90467453 158935 None 0 Human Functional pEC50 = 8.4 8.4 3 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4094794 158935 None 0 Human Functional pEC50 = 8.4 8.4 3 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
681 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
681.0 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
940 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
947 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
DB00988 1465 None 47 Human Functional pEC50 = 8.4 8.4 -2 15
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
71449211 80472 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 522 9 2 8 5.0 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cccc(-c3noc(C)n3)c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
CHEMBL2146503 80472 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 522 9 2 8 5.0 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cccc(-c3noc(C)n3)c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
90467587 157485 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 570 10 2 6 5.5 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4078351 157485 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 570 10 2 6 5.5 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
24805285 184601 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 300 2 1 3 2.1 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CCNC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL484732 184601 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 300 2 1 3 2.1 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CCNC4=O 10.1016/j.bmcl.2009.03.015
681 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
681.0 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
940 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
947 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
DB00988 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
681 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
681.0 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
940 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
947 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
DB00988 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
11224283 133573 None 0 Human Functional pEC50 = 8.3 8.3 12 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 433 7 1 4 4.1 COc1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm049465g
CHEMBL370713 133573 None 0 Human Functional pEC50 = 8.3 8.3 12 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 433 7 1 4 4.1 COc1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm049465g
44443948 94260 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 2 4 1.8 CCCN1CCOC(c2ccc(O)c(N)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL249793 94260 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 2 4 1.8 CCCN1CCOC(c2ccc(O)c(N)c2)C1 10.1016/j.bmcl.2007.10.059
25093832 155970 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155970 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
90644230 111853 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 111853 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
164617783 184696 None 0 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 184696 None 0 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
25093832 155970 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155970 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25072632 111839 None 0 Human Functional pEC50 = 7.4 7.4 30 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111839 None 0 Human Functional pEC50 = 7.4 7.4 30 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
90644230 111853 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 111853 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
44438201 93660 None 1 Human Functional pEC50 = 7.4 7.4 -2 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246637 93660 None 1 Human Functional pEC50 = 7.4 7.4 -2 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25072632 111839 None 0 Human Functional pEC50 = 7.4 7.4 30 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111839 None 0 Human Functional pEC50 = 7.4 7.4 30 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
164916997 196206 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 592 10 0 4 6.3 CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5418819 196206 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 592 10 0 4 6.3 CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
164916997 196206 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 592 10 0 4 6.3 CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5418819 196206 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 592 10 0 4 6.3 CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
164609017 184531 None 0 Human Functional pEC50 = 6.4 6.4 6 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 184531 None 0 Human Functional pEC50 = 6.4 6.4 6 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
137640391 156797 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 156797 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
44427829 151342 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL396024 151342 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
25071691 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
25071691 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 7.4 7.4 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
145993700 167426 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294279 167426 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
44443944 94194 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 264 4 2 4 1.3 CCCN1CCOC(c2ccc(O)c(C(N)=O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL249357 94194 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 264 4 2 4 1.3 CCCN1CCOC(c2ccc(O)c(C(N)=O)c2)C1 10.1016/j.bmcl.2007.10.059
137642380 158599 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 158599 None 0 Human Functional pEC50 = 7.4 7.4 5 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
71462090 84627 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2158640 84627 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2221044 84627 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
168286426 193035 None 0 Human Functional pEC50 = 6.3 6.3 -5 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 193035 None 0 Human Functional pEC50 = 6.3 6.3 -5 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 193035 None 0 Human Functional pEC50 = 6.3 6.3 -5 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
11676873 9197 None 0 Human Functional pEC50 = 7.3 7.3 21 2
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm050729o
CHEMBL110365 9197 None 0 Human Functional pEC50 = 7.3 7.3 21 2
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm050729o
145993990 167450 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294577 167450 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
90644228 111849 None 0 Human Functional pEC50 = 8.3 8.3 5 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 111849 None 0 Human Functional pEC50 = 8.3 8.3 5 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90644228 111849 None 0 Human Functional pEC50 = 8.3 8.3 5 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 111849 None 0 Human Functional pEC50 = 8.3 8.3 5 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
164623991 185643 None 0 Human Functional pEC50 = 8.3 8.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 8.3 8.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164623991 185643 None 0 Human Functional pEC50 = 8.3 8.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 8.3 8.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 8.3 8.3 2 7
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2007.08.038
54562 3261 None 19 Human Functional pEC50 = 8.3 8.3 2 7
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2007.08.038
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.3 8.3 2 7
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2007.08.038
114876 12797 None 1 Human Functional pEC50 = 8.3 8.3 7 6
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
CHEMBL1188090 12797 None 1 Human Functional pEC50 = 8.3 8.3 7 6
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
CHEMBL545783 12797 None 1 Human Functional pEC50 = 8.3 8.3 7 6
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
681 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
681.0 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
940 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
947 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
DB00988 1465 None 47 Human Functional pEC50 = 8.3 8.3 -2 15
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
11154555 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555.0 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
681 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
681.0 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
940 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
947 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
DB00988 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
11154555 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555.0 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 800 None 50 Human Functional pEC50 = 8.2 8.2 -1 10
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
90644227 111843 None 0 Human Functional pEC50 = 8.2 8.2 91 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111843 None 0 Human Functional pEC50 = 8.2 8.2 91 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90644227 111843 None 0 Human Functional pEC50 = 8.2 8.2 91 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111843 None 0 Human Functional pEC50 = 8.2 8.2 91 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
137640203 157054 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 157054 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
137640203 157054 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 157054 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
52937875 61195 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765634 61195 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
5311189 207299 None 9 Human Functional pEC50 = 7.3 7.3 2 4
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
CHEMBL7549 207299 None 9 Human Functional pEC50 = 7.3 7.3 2 4
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
90467453 158935 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4094794 158935 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
90467453 158935 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4094794 158935 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
164623991 185643 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164623991 185643 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
172442773 195208 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 432 8 1 2 5.3 CN(C)C(=O)C(CCN[C@@H]1C[C@H]1c1ccc(Cl)cc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5398913 195208 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 432 8 1 2 5.3 CN(C)C(=O)C(CCN[C@@H]1C[C@H]1c1ccc(Cl)cc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
44443902 94500 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 207 2 1 3 1.8 CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL251215 94500 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 207 2 1 3 1.8 CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
164937988 195320 None 4 Human Functional pEC50 = 5.3 5.3 -407 5
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Functional pEC50 = 5.3 5.3 -407 5
Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
24936042 157681 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
24936042 157681 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
90644226 111842 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111842 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
172313129 196051 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 506 9 0 6 5.3 CCC1(CC)CC(OCCCN2CCN(c3cccc(C(F)(F)F)n3)CC2)(c2ccccn2)CCO1 10.1021/acs.jmedchem.3c00417
CHEMBL5415842 196051 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 506 9 0 6 5.3 CCC1(CC)CC(OCCCN2CCN(c3cccc(C(F)(F)F)n3)CC2)(c2ccccn2)CCO1 10.1021/acs.jmedchem.3c00417
90644226 111842 None 0 Human Functional pEC50 = 7.2 7.2 7 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111842 None 0 Human Functional pEC50 = 7.2 7.2 7 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
127047593 140118 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 457 6 1 4 5.2 O=C(NCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1cccc2ccccc12 10.1039/C5MD00590F
CHEMBL3800194 140118 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 457 6 1 4 5.2 O=C(NCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1cccc2ccccc12 10.1039/C5MD00590F
172439032 195309 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172439032 195309 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisAgonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
122181331 121938 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590082 121938 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
681 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
681.0 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
940 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
947 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
DB00988 1465 None 47 Human Functional pEC50 = 8.2 8.2 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
90466573 158628 None 0 Human Functional pEC50 = 8.2 8.2 16 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4091498 158628 None 0 Human Functional pEC50 = 8.2 8.2 16 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466573 158628 None 0 Human Functional pEC50 = 8.2 8.2 16 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4091498 158628 None 0 Human Functional pEC50 = 8.2 8.2 16 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
127047319 140019 None 0 Human Functional pEC50 = 8.2 8.2 6 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 421 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccccc1 10.1039/C5MD00590F
CHEMBL3799603 140019 None 0 Human Functional pEC50 = 8.2 8.2 6 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 421 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccccc1 10.1039/C5MD00590F
9826580 206431 None 4 Human Functional pEC50 = 8.2 8.2 14 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL69451 206431 None 4 Human Functional pEC50 = 8.2 8.2 14 2
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
9826580 206431 None 4 Human Functional pEC50 = 8.2 8.2 14 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1016/s0960-894x(03)00389-5
CHEMBL69451 206431 None 4 Human Functional pEC50 = 8.2 8.2 14 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1016/s0960-894x(03)00389-5
85470564 156915 None 0 Human Functional pEC50 = 8.2 8.2 37 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156915 None 0 Human Functional pEC50 = 8.2 8.2 37 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
127045795 140196 None 0 Human Functional pEC50 = 8.2 8.2 50 2
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 515 8 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(C(=O)O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3798504 140196 None 0 Human Functional pEC50 = 8.2 8.2 50 2
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 515 8 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(C(=O)O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800681 140196 None 0 Human Functional pEC50 = 8.2 8.2 50 2
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 515 8 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(C(=O)O)c2ccccc12 10.1039/C5MD00590F
127045796 140197 None 0 Human Functional pEC50 = 8.2 8.2 39 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 514 8 2 5 4.9 NC(=O)c1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3798211 140197 None 0 Human Functional pEC50 = 8.2 8.2 39 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 514 8 2 5 4.9 NC(=O)c1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800682 140197 None 0 Human Functional pEC50 = 8.2 8.2 39 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 514 8 2 5 4.9 NC(=O)c1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
127047640 140149 None 0 Human Functional pEC50 = 8.2 8.2 28 2
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 460 7 2 4 5.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]ccc12 10.1039/C5MD00590F
CHEMBL3800421 140149 None 0 Human Functional pEC50 = 8.2 8.2 28 2
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 460 7 2 4 5.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]ccc12 10.1039/C5MD00590F
90467020 158213 None 0 Human Functional pEC50 = 8.2 8.2 8 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4086944 158213 None 0 Human Functional pEC50 = 8.2 8.2 8 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
11518173 58521 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2ccccc12 10.1021/jm050729o
CHEMBL168357 58521 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2ccccc12 10.1021/jm050729o
168679651 195904 None 2 Human Functional pEC50 = 6.2 6.2 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 428 9 1 3 4.6 COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5412995 195904 None 2 Human Functional pEC50 = 6.2 6.2 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 428 9 1 3 4.6 COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
137644966 158586 None 0 Human Functional pEC50 = 7.2 7.2 14 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 158586 None 0 Human Functional pEC50 = 7.2 7.2 14 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
11533234 58972 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 487 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)[C@H]1CC[C@@H](c2ccccc2)CC1 10.1021/jm050729o
CHEMBL168948 58972 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 487 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)[C@H]1CC[C@@H](c2ccccc2)CC1 10.1021/jm050729o
137636460 156211 None 0 Human Functional pEC50 = 7.2 7.2 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 156211 None 0 Human Functional pEC50 = 7.2 7.2 9 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
25071066 111837 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111837 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
25071066 111837 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111837 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
44438237 93712 None 1 Human Functional pEC50 = 6.2 6.2 -3 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL246855 93712 None 1 Human Functional pEC50 = 6.2 6.2 -3 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
24837518 157854 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 312 3 0 1 6.4 CCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
CHEMBL4082631 157854 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 312 3 0 1 6.4 CCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
168273745 192917 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192917 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192917 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
90466716 161097 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099236 161097 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116199 161097 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
122181330 121937 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121937 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
10457321 102126 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Compound was evaluated for effective concentration required for stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsCompound was evaluated for effective concentration required for stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 467 6 1 4 4.2 COc1c(C(=O)NCCN2CCN(c3ccccc3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL30208 102126 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Compound was evaluated for effective concentration required for stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsCompound was evaluated for effective concentration required for stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 467 6 1 4 4.2 COc1c(C(=O)NCCN2CCN(c3ccccc3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
15232475 100655 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 495 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(C)c3C)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL29182 100655 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 495 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(C)c3C)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
137657115 159849 None 0 Human Functional pEC50 = 7.2 7.2 11 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159849 None 0 Human Functional pEC50 = 7.2 7.2 11 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
228 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
33 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
6005 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
6005.0 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
CHEMBL53 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
DB00714 445 None 20 Human Functional pEC50 = 8.2 8.2 -11 20
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
127046595 140068 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 457 6 1 4 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2ccccc12 10.1039/C5MD00590F
CHEMBL3799902 140068 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 457 6 1 4 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2ccccc12 10.1039/C5MD00590F
90466717 157002 None 0 Human Functional pEC50 = 8.1 8.1 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 157002 None 0 Human Functional pEC50 = 8.1 8.1 5 2
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
127046016 140200 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 461 7 2 5 4.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]cnc12 10.1039/C5MD00590F
CHEMBL3798331 140200 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 461 7 2 5 4.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]cnc12 10.1039/C5MD00590F
CHEMBL3800685 140200 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 461 7 2 5 4.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]cnc12 10.1039/C5MD00590F
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
25071385 159250 None 0 Human Functional pEC50 = 8.1 8.1 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 8.1 8.1 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
4420454 56275 None 2 Human Functional pEC50 = 8.1 8.1 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm800895v
CHEMBL162762 56275 None 2 Human Functional pEC50 = 8.1 8.1 - 1
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm800895v
25071385 159250 None 0 Human Functional pEC50 = 8.1 8.1 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 8.1 8.1 2 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137657115 159849 None 0 Human Functional pEC50 = 7.2 7.2 11 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159849 None 0 Human Functional pEC50 = 7.2 7.2 11 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
137658100 159710 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4103339 159710 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
137658100 159710 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4103339 159710 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
164626153 186484 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 186484 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL5085974 217493 None 0 Human Functional pEC50 = 6.1 6.1 -11 2
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None CN(C)C(=O)C(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
127047461 140174 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1CCCC2 10.1039/C5MD00590F
CHEMBL3800575 140174 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1CCCC2 10.1039/C5MD00590F
164916967 195989 None 2 Human Functional pEC50 = 7.1 7.1 45 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5414796 195989 None 2 Human Functional pEC50 = 7.1 7.1 45 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
122181331 121938 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590082 121938 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
137643951 158351 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 158351 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
9794475 94339 None 10 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCO[C@H](c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL250403 94339 None 10 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCO[C@H](c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
2 3261 None 19 Human Functional pEC50 = 8.1 8.1 2 7
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
54562 3261 None 19 Human Functional pEC50 = 8.1 8.1 2 7
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.1 8.1 2 7
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
681 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
681.0 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
940 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
947 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
DB00988 1465 None 47 Human Functional pEC50 = 8.1 8.1 -2 15
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
168290815 193082 None 0 Human Functional pEC50 = 6.1 6.1 -10 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 193082 None 0 Human Functional pEC50 = 6.1 6.1 -10 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 193082 None 0 Human Functional pEC50 = 6.1 6.1 -10 2
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
15232476 102121 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL30206 102121 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
25141536 56264 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 587 7 2 5 4.6 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL1627318 56264 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 587 7 2 5 4.6 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
27842480 172519 None 29 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4476784 172519 None 29 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assayAgonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
44443901 155083 None 22 Human Functional pEC50 = 6.1 6.1 8 2
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 179 1 2 3 1.1 Oc1cccc(C2CNCCO2)c1 10.1016/j.bmcl.2007.10.059
CHEMBL401328 155083 None 22 Human Functional pEC50 = 6.1 6.1 8 2
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 179 1 2 3 1.1 Oc1cccc(C2CNCCO2)c1 10.1016/j.bmcl.2007.10.059
154725484 176570 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 176570 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 176570 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
164624107 185828 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185828 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
44400519 133197 None 0 Human Functional pEC50 = 8.0 8.0 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 133197 None 0 Human Functional pEC50 = 8.0 8.0 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
90467020 158213 None 0 Human Functional pEC50 = 8.0 8.0 8 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4086944 158213 None 0 Human Functional pEC50 = 8.0 8.0 8 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
90467020 158213 None 0 Human Functional pEC50 = 8.0 8.0 8 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4086944 158213 None 0 Human Functional pEC50 = 8.0 8.0 8 2
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
681 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
681.0 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
940 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
947 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
DB00988 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
681 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
681.0 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
940 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
947 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
CHEMBL59 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
DB00988 1465 None 47 Human Functional pEC50 = 8.0 8.0 -2 15
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
137644833 158231 None 0 Human Functional pEC50 = 8.0 8.0 95 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 158231 None 0 Human Functional pEC50 = 8.0 8.0 95 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
137644833 158231 None 0 Human Functional pEC50 = 8.0 8.0 95 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 158231 None 0 Human Functional pEC50 = 8.0 8.0 95 2
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
2 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
2 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.0 8.0 2 7
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
164619170 185707 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164916967 195989 None 2 Human Functional pEC50 = 8.0 8.0 45 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5414796 195989 None 2 Human Functional pEC50 = 8.0 8.0 45 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
44400553 70803 None 0 Human Functional pEC50 = 8.0 8.0 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70803 None 0 Human Functional pEC50 = 8.0 8.0 2 2
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
5311189 207299 None 9 Human Functional pEC50 = 8.0 8.0 2 4
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 207299 None 9 Human Functional pEC50 = 8.0 8.0 2 4
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
164619170 185707 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164916967 195989 None 2 Human Functional pEC50 = 8.0 8.0 45 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5414796 195989 None 2 Human Functional pEC50 = 8.0 8.0 45 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
133633 2241 None 40 Human Functional pEC50 = 7.0 7.0 -20 4
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
177 2241 None 40 Human Functional pEC50 = 7.0 7.0 -20 4
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
CHEMBL445102 2241 None 40 Human Functional pEC50 = 7.0 7.0 -20 4
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
172441436 195050 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 670 13 1 7 5.2 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2nsc3ccccc23)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5395539 195050 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 670 13 1 7 5.2 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2nsc3ccccc23)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
90467452 158532 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4090459 158532 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
90467452 158532 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4090459 158532 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
164619127 185631 None 0 Human Functional pEC50 = 7.0 7.0 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.0 7.0 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164619127 185631 None 0 Human Functional pEC50 = 7.0 7.0 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.0 7.0 -11 3
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
168475887 195235 None 2 Human Functional pEC50 = 7.0 7.0 10 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
CHEMBL5399270 195235 None 2 Human Functional pEC50 = 7.0 7.0 10 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
168475887 195235 None 2 Human Functional pEC50 = 7.0 7.0 10 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
CHEMBL5399270 195235 None 2 Human Functional pEC50 = 7.0 7.0 10 2
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assayPartial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
44438236 154990 None 1 Human Functional pEC50 = 7.0 7.0 -4 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL400827 154990 None 1 Human Functional pEC50 = 7.0 7.0 -4 2
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
154706030 176650 None 1 Human Functional pEC50 = 7 7.0 35 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 176650 None 1 Human Functional pEC50 = 7 7.0 35 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 176650 None 1 Human Functional pEC50 = 7 7.0 35 2
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
9888555 165699 None 19 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 165699 None 19 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
73671217 113750 None 0 Human Functional pIC50 = 9.5 9.5 27 2
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 504 7 1 8 3.2 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccncc4n3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
CHEMBL3323016 113750 None 0 Human Functional pIC50 = 9.5 9.5 27 2
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 504 7 1 8 3.2 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccncc4n3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
25130157 103362 None 0 Human Functional pIC50 = 9.1 9.1 2 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 103362 None 0 Human Functional pIC50 = 9.1 9.1 2 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
44427820 93252 None 0 Human Functional pIC50 = 9 9.0 40 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 496 7 2 4 4.5 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc(=O)[nH]2)cc1 10.1021/jm0704200
CHEMBL244562 93252 None 0 Human Functional pIC50 = 9 9.0 40 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 496 7 2 4 4.5 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc(=O)[nH]2)cc1 10.1021/jm0704200
11223885 70723 None 0 Human Functional pIC50 = 9 9.0 8 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 419 6 2 4 3.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(O)cc1 10.1021/jm040190e
CHEMBL195057 70723 None 0 Human Functional pIC50 = 9 9.0 8 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 419 6 2 4 3.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(O)cc1 10.1021/jm040190e
42625207 56250 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627304 56250 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
44427823 93276 None 0 Human Functional pIC50 = 8.9 8.9 60 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1 10.1021/jm0704200
CHEMBL244774 93276 None 0 Human Functional pIC50 = 8.9 8.9 60 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1 10.1021/jm0704200
66574145 113745 None 0 Human Functional pIC50 = 8.9 8.9 81 2
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
CHEMBL3323011 113745 None 0 Human Functional pIC50 = 8.9 8.9 81 2
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
86342156 149686 None 0 Human Functional pIC50 = 8.9 8.9 22 4
Antagonistic activity at D3 receptor (unknown origin) expressed in cell membranes assessed as inhibition of quinpirole-induced response after 40 mins by [35S]GTPgammaS binding assayAntagonistic activity at D3 receptor (unknown origin) expressed in cell membranes assessed as inhibition of quinpirole-induced response after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 438 6 1 6 4.4 O=C(N[C@H]1CC[C@H](CCN2CCN(c3nsc4ccccc34)CC2)CC1)c1ccco1 10.1016/j.ejmech.2016.07.038
CHEMBL3946995 149686 None 0 Human Functional pIC50 = 8.9 8.9 22 4
Antagonistic activity at D3 receptor (unknown origin) expressed in cell membranes assessed as inhibition of quinpirole-induced response after 40 mins by [35S]GTPgammaS binding assayAntagonistic activity at D3 receptor (unknown origin) expressed in cell membranes assessed as inhibition of quinpirole-induced response after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 438 6 1 6 4.4 O=C(N[C@H]1CC[C@H](CCN2CCN(c3nsc4ccccc34)CC2)CC1)c1ccco1 10.1016/j.ejmech.2016.07.038
42626172 56260 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm900095y
CHEMBL1627314 56260 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm900095y
42626381 56261 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
CHEMBL1627315 56261 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
25141538 56257 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 56257 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
3038495 708 None 33 Human Functional pIC50 = 8.7 8.7 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 708 None 33 Human Functional pIC50 = 8.7 8.7 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 708 None 33 Human Functional pIC50 = 8.7 8.7 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
172454491 195657 None 0 Human Functional pIC50 = 8.7 8.7 3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5408223 195657 None 0 Human Functional pIC50 = 8.7 8.7 3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
172454491 195657 None 0 Human Functional pIC50 = 8.7 8.7 3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5408223 195657 None 0 Human Functional pIC50 = 8.7 8.7 3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
11154555 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
11154555.0 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
5037 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
7671 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL2028019 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL3085826 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
DB06016 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
25132869 103350 None 0 Human Functional pIC50 = 8.0 8.0 20 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 103350 None 0 Human Functional pIC50 = 8.0 8.0 20 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
42626313 56263 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627317 56263 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
44309688 206450 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
CHEMBL69571 206450 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
53248260 62059 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 454 9 2 5 3.5 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774540 62059 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 454 9 2 5 3.5 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
172464337 196969 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
25141535 56254 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627308 56254 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
172464337 196969 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
25129807 103349 None 0 Human Functional pIC50 = 7.9 7.9 3 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084502 103349 None 0 Human Functional pIC50 = 7.9 7.9 3 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
44427831 92291 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL242644 92291 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
171492372 197072 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
171492372 197072 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
53248213 62054 None 0 Human Functional pIC50 = 5.9 5.9 2 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 62054 None 0 Human Functional pIC50 = 5.9 5.9 2 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
53248210 62051 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774532 62051 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
164937996 197036 None 0 Human Functional pIC50 = 4.9 4.9 -977 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccnc(N2CCN(CCCc3nc4ccccc4s3)CC2)c1 10.1021/acs.jmedchem.3c00734
CHEMBL5437265 197036 None 0 Human Functional pIC50 = 4.9 4.9 -977 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccnc(N2CCN(CCCc3nc4ccccc4s3)CC2)c1 10.1021/acs.jmedchem.3c00734
37459 746 None 9 Human Functional pIC50 = 7.9 7.9 -13 4
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysisAntagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/acs.jmedchem.3c00976
62 746 None 9 Human Functional pIC50 = 7.9 7.9 -13 4
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysisAntagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/acs.jmedchem.3c00976
CHEMBL8514 746 None 9 Human Functional pIC50 = 7.9 7.9 -13 4
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysisAntagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/acs.jmedchem.3c00976
172454049 195686 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 450 7 1 4 4.3 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5409134 195686 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 450 7 1 4 4.3 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172454049 195686 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 450 7 1 4 4.3 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5409134 195686 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 450 7 1 4 4.3 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
42625290 56262 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL1627316 56262 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
164938002 194980 None 0 Human Functional pIC50 = 4.9 4.9 -218 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 351 5 0 4 4.8 Cc1cccnc1C1CCN(CCCc2nc3ccccc3s2)CC1 10.1021/acs.jmedchem.3c00734
CHEMBL5394387 194980 None 0 Human Functional pIC50 = 4.9 4.9 -218 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 351 5 0 4 4.8 Cc1cccnc1C1CCN(CCCc2nc3ccccc3s2)CC1 10.1021/acs.jmedchem.3c00734
44427841 86173 None 0 Human Functional pIC50 = 7.8 7.8 21 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL231156 86173 None 0 Human Functional pIC50 = 7.8 7.8 21 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
6674 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
9891901 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
CHEMBL300780 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
6674 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
9891901 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL300780 2817 None 23 Human Functional pIC50 = 7.8 7.8 151 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
42625293 56265 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 56265 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
42625205 56270 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627324 56270 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
11696813 188024 None 9 Human Functional pIC50 = 6.8 6.8 5 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
CHEMBL496739 188024 None 9 Human Functional pIC50 = 6.8 6.8 5 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
53248211 62052 None 0 Human Functional pIC50 = 5.8 5.8 1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 493 8 1 5 5.0 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774533 62052 None 0 Human Functional pIC50 = 5.8 5.8 1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 493 8 1 5 5.0 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm200288r
60165418 75375 None 0 Human Functional pIC50 = 5.8 5.8 -9 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL2037521 75375 None 0 Human Functional pIC50 = 5.8 5.8 -9 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
168475866 196686 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 455 11 2 6 5.1 CCCCCCOc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OCCOCC)c3CN1CC2 10.1021/acs.jmedchem.3c00976
CHEMBL5429932 196686 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 455 11 2 6 5.1 CCCCCCOc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OCCOCC)c3CN1CC2 10.1021/acs.jmedchem.3c00976
56852956 112106 None 1 Human Functional pIC50 = 4.8 4.8 -281 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL3289656 112106 None 1 Human Functional pIC50 = 4.8 4.8 -281 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5075990 216895 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
164938010 195433 None 0 Human Functional pIC50 = 4.8 4.8 -117 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5403610 195433 None 0 Human Functional pIC50 = 4.8 4.8 -117 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
37459 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levelsAntagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levels
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.ejmech.2014.12.045
62 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levelsAntagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levels
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.ejmech.2014.12.045
CHEMBL8514 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levelsAntagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levels
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.ejmech.2014.12.045
37459 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/jm401895u
62 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/jm401895u
CHEMBL8514 746 None 9 Human Functional pIC50 = 7.8 7.8 -13 4
Antagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1021/jm401895u
53248259 62058 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 479 7 1 4 5.5 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm200288r
CHEMBL1774539 62058 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 479 7 1 4 5.5 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm200288r
172459790 196485 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172459790 196485 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
42626380 56259 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627313 56259 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
44309775 102733 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
CHEMBL304605 102733 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
172444851 195152 None 0 Human Functional pIC50 = 5.8 5.8 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 474 10 0 2 6.4 CCCN(CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1)[C@@H]1C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00417
CHEMBL5397609 195152 None 0 Human Functional pIC50 = 5.8 5.8 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 474 10 0 2 6.4 CCCN(CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1)[C@@H]1C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.3c00417
42626318 56252 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627306 56252 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
11408148 128788 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 128788 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
11408148 128788 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL366904 128788 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44427826 93326 None 0 Human Functional pIC50 = 7.7 7.7 9 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 453 7 1 4 4.4 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL244989 93326 None 0 Human Functional pIC50 = 7.7 7.7 9 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 453 7 1 4 4.4 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
73670899 113779 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 545 8 1 5 5.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)[C@H]3CC[C@H](c4ccccc4)CC3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
CHEMBL3323117 113779 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by dopamine potency shift assay
ChEMBL 545 8 1 5 5.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)[C@H]3CC[C@H](c4ccccc4)CC3)CC2)cc(C(F)(F)F)n1 10.1021/jm500801r
172468596 197053 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5437660 197053 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172468596 197053 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5437660 197053 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5080654 217186 None 0 Human Functional pIC50 = 5.7 5.7 -134 2
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1021/acs.jmedchem.1c00611
11154555 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
11154555.0 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
5037 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
7671 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL2028019 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL3085826 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
DB06016 800 None 50 Human Functional pIC50 = 8.7 8.7 -1 10
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.2c01624
11676873 9197 None 0 Human Functional pIC50 = 8.7 8.7 21 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL110365 9197 None 0 Human Functional pIC50 = 8.7 8.7 21 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
11316847 70371 None 0 Human Functional pIC50 = 8.7 8.7 6 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm040190e
CHEMBL194493 70371 None 0 Human Functional pIC50 = 8.7 8.7 6 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm040190e
10092819 16780 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL124444 16780 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
1353 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
3559 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
3559.0 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
86 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL54 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
DB00502 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
1353 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
3559 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
3559.0 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
86 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
CHEMBL54 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
DB00502 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.2c01624
1353 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
3559 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
3559.0 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
86 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
CHEMBL54 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
DB00502 1911 None 63 Human Functional pIC50 = 8.6 8.6 2 39
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.3c00417
44427818 92157 None 0 Human Functional pIC50 = 8.5 8.5 38 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 444 9 1 5 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL241973 92157 None 0 Human Functional pIC50 = 8.5 8.5 38 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 444 9 1 5 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
53248256 62055 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
CHEMBL1774536 62055 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
25141536 56264 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 587 7 2 5 4.6 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL1627318 56264 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 587 7 2 5 4.6 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
44393403 65099 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 65099 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
164937988 195320 None 4 Human Functional pIC50 = 4.7 4.7 -407 5
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Functional pIC50 = 4.7 4.7 -407 5
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
42626243 56256 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 478 7 3 4 3.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(F)ccc2[nH]1 10.1021/jm900095y
CHEMBL1627310 56256 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 478 7 3 4 3.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(F)ccc2[nH]1 10.1021/jm900095y
2389 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
5073 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
5073.0 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
96 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
CHEMBL85 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
DB00734 3331 None 72 Human Functional pIC50 = 7.6 7.6 -24 29
Antagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assayAntagonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as inhibition of dopamine-induced beta-arrestin translocation activity preincubated for 30 mins followed by dopamine addition and measured after 90 to 180 min by pathHunter microplate based TANGO assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.3c00976
11307083 63576 None 0 Human Functional pIC50 = 7.6 7.6 6 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm040190e
CHEMBL180060 63576 None 0 Human Functional pIC50 = 7.6 7.6 6 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm040190e
164937986 195324 None 0 Human Functional pIC50 = 4.6 4.6 -42 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 372 5 0 5 4.1 Clc1ccc2sc(CCCN3CCN(c4ccccn4)CC3)nc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5400983 195324 None 0 Human Functional pIC50 = 4.6 4.6 -42 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 372 5 0 5 4.1 Clc1ccc2sc(CCCN3CCN(c4ccccn4)CC3)nc2c1 10.1021/acs.jmedchem.3c00734
129103318 167410 None 0 Human Functional pIC50 = 7.6 7.6 -2 6
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167410 None 0 Human Functional pIC50 = 7.6 7.6 -2 6
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
44427822 93275 None 0 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.5 Cc1cccnc1-c1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm0704200
CHEMBL244773 93275 None 0 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.5 Cc1cccnc1-c1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm0704200
42625295 56267 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627321 56267 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
53248298 62061 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 473 7 1 3 5.4 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm200288r
CHEMBL1774542 62061 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 473 7 1 3 5.4 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm200288r
53248159 62009 None 0 Human Functional pIC50 = 6.6 6.6 4 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 62009 None 0 Human Functional pIC50 = 6.6 6.6 4 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
24769156 116281 None 0 Human Functional pIC50 = 6.6 6.6 6 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as reduction in dopamine-induced response by [35S]GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as reduction in dopamine-induced response by [35S]GTPgammaS binding assay
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
CHEMBL3358509 116281 None 0 Human Functional pIC50 = 6.6 6.6 6 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as reduction in dopamine-induced response by [35S]GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as reduction in dopamine-induced response by [35S]GTPgammaS binding assay
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
44309509 96573 None 0 Human Functional pIC50 = 7.6 7.6 2 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 457 7 1 5 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2n1 10.1021/jm040190e
CHEMBL262724 96573 None 0 Human Functional pIC50 = 7.6 7.6 2 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 457 7 1 5 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2n1 10.1021/jm040190e
44309509 96573 None 0 Human Functional pIC50 = 7.6 7.6 2 2
Antagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAntagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 457 7 1 5 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2n1 10.1016/s0960-894x(03)00389-5
CHEMBL262724 96573 None 0 Human Functional pIC50 = 7.6 7.6 2 2
Antagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAntagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 457 7 1 5 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2n1 10.1016/s0960-894x(03)00389-5
168475887 195235 None 2 Human Functional pIC50 = 6.6 6.6 10 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
CHEMBL5399270 195235 None 2 Human Functional pIC50 = 6.6 6.6 10 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 419 5 0 4 4.6 Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl 10.1021/acs.jmedchem.3c00417
168475888 196855 None 2 Human Functional pIC50 = 6.6 6.6 -1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 410 6 1 3 5.6 Clc1ccc([C@@H]2C[C@H]2NCCC2(c3ccccn3)CCOC3(CCCC3)C2)cc1 10.1021/acs.jmedchem.3c00417
CHEMBL5433458 196855 None 2 Human Functional pIC50 = 6.6 6.6 -1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 410 6 1 3 5.6 Clc1ccc([C@@H]2C[C@H]2NCCC2(c3ccccn3)CCOC3(CCCC3)C2)cc1 10.1021/acs.jmedchem.3c00417
164938006 195571 None 0 Human Functional pIC50 = 5.6 5.6 -53 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1cccc2nc(CCCN3CCC(c4ccccn4)CC3)sc12 10.1021/acs.jmedchem.3c00734
CHEMBL5406300 195571 None 0 Human Functional pIC50 = 5.6 5.6 -53 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1cccc2nc(CCCN3CCC(c4ccccn4)CC3)sc12 10.1021/acs.jmedchem.3c00734
25141534 56251 None 0 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 56251 None 0 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
164916968 196909 None 0 Human Functional pIC50 = 5.5 5.5 12 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
CHEMBL5434650 196909 None 0 Human Functional pIC50 = 5.5 5.5 12 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 618 11 1 6 4.9 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.3c00417
53248260 62059 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 454 9 2 5 3.5 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774540 62059 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 454 9 2 5 3.5 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
11477180 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
6675 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
CHEMBL180010 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
3038495 708 None 33 Human Functional pIC50 = 8.5 8.5 -8 8
Partial agonist intrinsic activity at dopamine D3 receptorPartial agonist intrinsic activity at dopamine D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 708 None 33 Human Functional pIC50 = 8.5 8.5 -8 8
Partial agonist intrinsic activity at dopamine D3 receptorPartial agonist intrinsic activity at dopamine D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 708 None 33 Human Functional pIC50 = 8.5 8.5 -8 8
Partial agonist intrinsic activity at dopamine D3 receptorPartial agonist intrinsic activity at dopamine D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
11477180 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
6675 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL180010 3074 None 4 Human Functional pIC50 = 8.5 8.5 26 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
172467420 196886 None 0 Human Functional pIC50 = 8.5 8.5 8 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5434229 196886 None 0 Human Functional pIC50 = 8.5 8.5 8 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
172467420 196886 None 0 Human Functional pIC50 = 8.5 8.5 8 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5434229 196886 None 0 Human Functional pIC50 = 8.5 8.5 8 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
1353 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
3559 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
3559.0 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
86 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
CHEMBL54 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
DB00502 1911 None 63 Human Functional pIC50 = 8.5 8.5 2 39
Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assayAntagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
44309510 102177 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 531 7 1 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm040190e
CHEMBL302374 102177 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 531 7 1 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm040190e
172449716 195885 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 682 13 1 6 5.0 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5412606 195885 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 682 13 1 6 5.0 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
53248261 62060 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 492 8 2 4 4.8 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774541 62060 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 492 8 2 4 4.8 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm200288r
53248258 62057 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
CHEMBL1774538 62057 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
171492463 197008 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 511 6 1 5 5.2 O=C(N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1)c1ccnc2ccccc12 10.1021/acs.jmedchem.2c01624
CHEMBL5436641 197008 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 511 6 1 5 5.2 O=C(N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1)c1ccnc2ccccc12 10.1021/acs.jmedchem.2c01624
171492463 197008 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 511 6 1 5 5.2 O=C(N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1)c1ccnc2ccccc12 10.1021/acs.jmedchem.2c01624
CHEMBL5436641 197008 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 511 6 1 5 5.2 O=C(N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1)c1ccnc2ccccc12 10.1021/acs.jmedchem.2c01624
171492376 195452 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5404054 195452 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
171492376 195452 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5404054 195452 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
53248259 62058 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 479 7 1 4 5.5 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm200288r
CHEMBL1774539 62058 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 479 7 1 4 5.5 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm200288r
42626171 56258 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 586 7 3 4 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2[nH]1 10.1021/jm900095y
CHEMBL1627312 56258 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 586 7 3 4 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2[nH]1 10.1021/jm900095y
164916930 195492 None 0 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 680 13 2 7 4.0 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5404724 195492 None 0 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 680 13 2 7 4.0 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
42626315 56266 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627320 56266 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
53248158 62008 None 0 Human Functional pIC50 = 6.4 6.4 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
CHEMBL1774383 62008 None 0 Human Functional pIC50 = 6.4 6.4 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
25128757 103359 None 0 Human Functional pIC50 = 8.4 8.4 6 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 103359 None 0 Human Functional pIC50 = 8.4 8.4 6 2
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
169410194 196730 None 6 Human Functional pIC50 = 8.3 8.3 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pIC50 = 8.3 8.3 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
169410194 196730 None 6 Human Functional pIC50 = 8.3 8.3 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pIC50 = 8.3 8.3 -1 2
Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysisAntagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
11224283 133573 None 0 Human Functional pIC50 = 8.3 8.3 12 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 433 7 1 4 4.1 COc1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm040190e
CHEMBL370713 133573 None 0 Human Functional pIC50 = 8.3 8.3 12 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 433 7 1 4 4.1 COc1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1021/jm040190e
10276451 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
10276451 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 202741 None 32 Human Functional pIC50 = 8.3 8.3 19 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
44427825 149466 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 442 8 1 5 3.9 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL394541 149466 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 442 8 1 5 3.9 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
53248209 62011 None 3 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
CHEMBL1774386 62011 None 3 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
53248208 62010 None 0 Human Functional pIC50 = 6.4 6.4 -3 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
CHEMBL1774385 62010 None 0 Human Functional pIC50 = 6.4 6.4 -3 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
172446093 195429 None 0 Human Functional pIC50 = 6.3 6.3 -58 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 368 6 0 6 3.5 COc1cccnc1N1CCN(CCCc2nc3ccccc3s2)CC1 10.1021/acs.jmedchem.3c00734
CHEMBL5403504 195429 None 0 Human Functional pIC50 = 6.3 6.3 -58 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 368 6 0 6 3.5 COc1cccnc1N1CCN(CCCc2nc3ccccc3s2)CC1 10.1021/acs.jmedchem.3c00734
25141534 56251 None 0 Human Functional pIC50 = 6.3 6.3 7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1627305 56251 None 0 Human Functional pIC50 = 6.3 6.3 7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
6674 2817 None 23 Human Functional pIC50 = 8.3 8.3 151 2
Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorAntagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
9891901 2817 None 23 Human Functional pIC50 = 8.3 8.3 151 2
Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorAntagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL300780 2817 None 23 Human Functional pIC50 = 8.3 8.3 151 2
Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorAntagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
44427836 144048 None 0 Human Functional pIC50 = 8.3 8.3 20 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL390253 144048 None 0 Human Functional pIC50 = 8.3 8.3 20 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
44309876 206329 None 0 Human Functional pIC50 = 7.3 7.3 10 2
Antagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAntagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 462 7 2 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(F)ccc2[nH]1 10.1016/s0960-894x(03)00389-5
CHEMBL68740 206329 None 0 Human Functional pIC50 = 7.3 7.3 10 2
Antagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAntagonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 462 7 2 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(F)ccc2[nH]1 10.1016/s0960-894x(03)00389-5
10438027 66209 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 66209 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
53248213 62054 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 62054 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
172442773 195208 None 0 Human Functional pIC50 = 5.3 5.3 -6 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 432 8 1 2 5.3 CN(C)C(=O)C(CCN[C@@H]1C[C@H]1c1ccc(Cl)cc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5398913 195208 None 0 Human Functional pIC50 = 5.3 5.3 -6 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 432 8 1 2 5.3 CN(C)C(=O)C(CCN[C@@H]1C[C@H]1c1ccc(Cl)cc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
3038495 708 None 33 Human Functional pIC50 = 7.3 7.3 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 708 None 33 Human Functional pIC50 = 7.3 7.3 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 708 None 33 Human Functional pIC50 = 7.3 7.3 -8 8
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
1577 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
2537 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
5355 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
5501 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
643497 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
688272 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
688272.0 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
958 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
960 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL196677 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL26 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL267044 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
DB00391 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
DB16021 3703 None 66 Human Functional pIC50 = 6.3 6.3 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
172313129 196051 None 0 Human Functional pIC50 = 6.3 6.3 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 506 9 0 6 5.3 CCC1(CC)CC(OCCCN2CCN(c3cccc(C(F)(F)F)n3)CC2)(c2ccccn2)CCO1 10.1021/acs.jmedchem.3c00417
CHEMBL5415842 196051 None 0 Human Functional pIC50 = 6.3 6.3 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 506 9 0 6 5.3 CCC1(CC)CC(OCCCN2CCN(c3cccc(C(F)(F)F)n3)CC2)(c2ccccn2)CCO1 10.1021/acs.jmedchem.3c00417
168475866 196686 None 2 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysisAntagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
ChEMBL 455 11 2 6 5.1 CCCCCCOc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OCCOCC)c3CN1CC2 10.1021/acs.jmedchem.3c00976
CHEMBL5429932 196686 None 2 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysisAntagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
ChEMBL 455 11 2 6 5.1 CCCCCCOc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OCCOCC)c3CN1CC2 10.1021/acs.jmedchem.3c00976
9887463 206845 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C\CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1016/s0960-894x(03)00389-5
CHEMBL71865 206845 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C\CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1016/s0960-894x(03)00389-5
9887463 206845 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C\CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm040190e
CHEMBL71865 206845 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C\CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm040190e
9826580 206431 None 4 Human Functional pIC50 = 8.2 8.2 14 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm040190e
CHEMBL69451 206431 None 4 Human Functional pIC50 = 8.2 8.2 14 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm040190e
42625211 56255 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627309 56255 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
42626240 56253 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627307 56253 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
44427821 153822 None 0 Human Functional pIC50 = 8.2 8.2 190 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.5 Cc1cccc(-c2ccc(C(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)n1 10.1021/jm0704200
CHEMBL398175 153822 None 0 Human Functional pIC50 = 8.2 8.2 190 2
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAntagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 494 7 1 4 5.5 Cc1cccc(-c2ccc(C(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)n1 10.1021/jm0704200
168679651 195904 None 2 Human Functional pIC50 = 6.2 6.2 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 428 9 1 3 4.6 COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5412995 195904 None 2 Human Functional pIC50 = 6.2 6.2 1 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 428 9 1 3 4.6 COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
164622805 185969 None 0 Human Functional pIC50 = 7.2 7.2 -5 6
Antagonist activity at D3 receptor (unknown origin)Antagonist activity at D3 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185969 None 0 Human Functional pIC50 = 7.2 7.2 -5 6
Antagonist activity at D3 receptor (unknown origin)Antagonist activity at D3 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
1577 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
2537 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
5355 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
5501 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
643497 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
688272 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
688272.0 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
958 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
960 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL196677 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL26 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
CHEMBL267044 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
DB00391 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
DB16021 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm200288r
164937992 195263 None 0 Human Functional pIC50 = 5.2 5.2 -45 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 351 5 0 4 4.8 Cc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5399689 195263 None 0 Human Functional pIC50 = 5.2 5.2 -45 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 351 5 0 4 4.8 Cc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
1577 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
2537 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
5355 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
5501 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
643497 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
688272 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
688272.0 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
958 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
960 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
CHEMBL196677 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
CHEMBL26 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
CHEMBL267044 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
DB00391 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
DB16021 3703 None 66 Human Functional pIC50 = 7.2 7.2 -3 8
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/acs.jmedchem.3c00734
53248158 62008 None 0 Human Functional pIC50 = 6.2 6.2 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
CHEMBL1774383 62008 None 0 Human Functional pIC50 = 6.2 6.2 -7 2
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assayAntagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
42626103 56269 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 56269 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
10001256 206749 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm040190e
CHEMBL71327 206749 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 403 6 1 3 4.1 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm040190e
53248210 62051 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774532 62051 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
164916967 195989 None 2 Human Functional pIC50 = 7.1 7.1 45 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5414796 195989 None 2 Human Functional pIC50 = 7.1 7.1 45 2
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 679 13 2 6 4.9 CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
53248257 62056 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 511 7 1 3 5.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm200288r
CHEMBL1774537 62056 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 511 7 1 3 5.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm200288r
53248212 62053 None 0 Human Functional pIC50 = 6.1 6.1 1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 62053 None 0 Human Functional pIC50 = 6.1 6.1 1 2
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
53248258 62057 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
CHEMBL1774538 62057 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
164937998 196922 None 0 Human Functional pIC50 = 5.1 5.1 -35 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc(C2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5434856 196922 None 0 Human Functional pIC50 = 5.1 5.1 -35 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc(C2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
172439985 195264 None 0 Human Functional pIC50 = 5.1 5.1 -35 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5399720 195264 None 0 Human Functional pIC50 = 5.1 5.1 -35 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
9980998 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
9980998 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 31043 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
11351639 60544 None 0 Human Functional pIC50 = 8.0 8.0 26 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 60544 None 0 Human Functional pIC50 = 8.0 8.0 26 2
Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesisAntagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
11351639 60544 None 0 Human Functional pIC50 = 8.0 8.0 26 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL175734 60544 None 0 Human Functional pIC50 = 8.0 8.0 26 2
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptorMitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
133633 2241 None 40 Human Functional pIC50 = 7.0 7.0 -20 4
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 2241 None 40 Human Functional pIC50 = 7.0 7.0 -20 4
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 2241 None 40 Human Functional pIC50 = 7.0 7.0 -20 4
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
172441436 195050 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 670 13 1 7 5.2 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2nsc3ccccc23)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
CHEMBL5395539 195050 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assayAntagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay
ChEMBL 670 13 1 7 5.2 CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2nsc3ccccc23)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c00417
53248395 61803 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 511 8 0 3 6.5 CN(CCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)Cc1ccc2c(c1)Cc1ccccc1-2 10.1021/jm200288r
CHEMBL1773087 61803 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
ChEMBL 511 8 0 3 6.5 CN(CCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)Cc1ccc2c(c1)Cc1ccccc1-2 10.1021/jm200288r
2470 3653 None 40 Human Functional pIC50 = 7.0 7.0 -213 23
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.8b01096
3300 3653 None 40 Human Functional pIC50 = 7.0 7.0 -213 23
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.8b01096
5265 3653 None 40 Human Functional pIC50 = 7.0 7.0 -213 23
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.8b01096
99 3653 None 40 Human Functional pIC50 = 7.0 7.0 -213 23
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.8b01096
CHEMBL267930 3653 None 40 Human Functional pIC50 = 7.0 7.0 -213 23
Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.8b01096
164937983 196526 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 366 6 0 5 4.1 Cc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5425920 196526 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAntagonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 366 6 0 5 4.1 Cc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
71452041 1944 None 4 Human Functional pIC50 = 6.0 6.0 -72 3
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 309 8 1 2 4.3 Oc1cccc(c1)CCN(CC1CCC1)CCc1ccccc1 10.1021/jm301258w
9189 1944 None 4 Human Functional pIC50 = 6.0 6.0 -72 3
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 309 8 1 2 4.3 Oc1cccc(c1)CCN(CC1CCC1)CCc1ccccc1 10.1021/jm301258w
CHEMBL2180639 1944 None 4 Human Functional pIC50 = 6.0 6.0 -72 3
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAntagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 309 8 1 2 4.3 Oc1cccc(c1)CCN(CC1CCC1)CCc1ccccc1 10.1021/jm301258w
11016342 102859 None 0 Human Functional pKd = 9.0 9.0 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm050729o
CHEMBL305362 102859 None 0 Human Functional pKd = 9.0 9.0 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm050729o
6674 2817 None 23 Human Functional pKd = 8.7 8.7 151 2
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm050729o
9891901 2817 None 23 Human Functional pKd = 8.7 8.7 151 2
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm050729o
CHEMBL300780 2817 None 23 Human Functional pKd = 8.7 8.7 151 2
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm050729o
3038495 708 None 33 Human Functional pKd = 7.8 7.8 -8 8
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050729o
7625 708 None 33 Human Functional pKd = 7.8 7.8 -8 8
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050729o
CHEMBL25236 708 None 33 Human Functional pKd = 7.8 7.8 -8 8
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050729o
11533234 123205 None 0 Human Functional pKd = 7.6 7.6 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 487 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)[C@H]1CC[C@H](c2ccccc2)CC1 10.1021/jm050729o
CHEMBL361228 123205 None 0 Human Functional pKd = 7.6 7.6 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 487 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)[C@H]1CC[C@H](c2ccccc2)CC1 10.1021/jm050729o
10939408 47437 None 0 Human Functional pKd = 8.5 8.5 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm050729o
CHEMBL154508 47437 None 0 Human Functional pKd = 8.5 8.5 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm050729o
1353 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
3559 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
3559.0 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
86 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
CHEMBL54 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
DB00502 1911 None 63 Human Functional pKd = 6.5 6.5 2 39
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm050729o
10939167 9502 None 0 Human Functional pKd = 7.4 7.4 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm050729o
CHEMBL112065 9502 None 0 Human Functional pKd = 7.4 7.4 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm050729o
CHEMBL129483 9502 None 0 Human Functional pKd = 7.4 7.4 - 1
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm050729o
11510684 166278 None 0 Human Functional pKd = 8.1 8.1 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
CHEMBL426414 166278 None 0 Human Functional pKd = 8.1 8.1 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
11647384 59123 None 0 Human Functional pKd = 7.1 7.1 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccccc23)CC1 10.1021/jm050729o
CHEMBL169766 59123 None 0 Human Functional pKd = 7.1 7.1 - 0
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccccc23)CC1 10.1021/jm050729o
121304452 149006 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3941818 149006 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
121304452 149006 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3941818 149006 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
57533 206397 None 31 Human Functional pKi = 9.7 9.7 - 1
Agonistic activity at DRD3 receptorAgonistic activity at DRD3 receptor
ChEMBL 247 2 1 3 2.5 CCCN1CCO[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.07.055
CHEMBL1288585 206397 None 31 Human Functional pKi = 9.7 9.7 - 1
Agonistic activity at DRD3 receptorAgonistic activity at DRD3 receptor
ChEMBL 247 2 1 3 2.5 CCCN1CCO[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.07.055
CHEMBL2106804 206397 None 31 Human Functional pKi = 9.7 9.7 - 1
Agonistic activity at DRD3 receptorAgonistic activity at DRD3 receptor
ChEMBL 247 2 1 3 2.5 CCCN1CCO[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.07.055
CHEMBL69271 206397 None 31 Human Functional pKi = 9.7 9.7 - 1
Agonistic activity at DRD3 receptorAgonistic activity at DRD3 receptor
ChEMBL 247 2 1 3 2.5 CCCN1CCO[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.07.055
44627351 6257 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081587 6257 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
11272440 6276 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.1 Cc1ccc2c(-c3nnc(SCCCN4C[C@@H]5C[C@]5(c5ccc(C(F)(F)F)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081685 6276 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.1 Cc1ccc2c(-c3nnc(SCCCN4C[C@@H]5C[C@]5(c5ccc(C(F)(F)F)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
11397777 6290 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 7 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)s1 10.1021/jm901319p
CHEMBL1081746 6290 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 7 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)s1 10.1021/jm901319p
46881466 7265 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 327 3 1 2 3.1 O=C1N(CC2CCCCN2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1085903 7265 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 327 3 1 2 3.1 O=C1N(CC2CCCCN2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.01.090
11213136 5947 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079824 5947 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
121304527 147128 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 445 7 0 7 4.4 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3926847 147128 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 445 7 0 7 4.4 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
121304437 151055 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 478 7 0 5 6.2 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCCCC1 10.1021/acs.jmedchem.6b00972
CHEMBL3958201 151055 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 478 7 0 5 6.2 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCCCC1 10.1021/acs.jmedchem.6b00972
121304569 146298 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(-c2ncco2)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3920167 146298 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(-c2ncco2)c1 10.1021/acs.jmedchem.6b00972
121304408 143641 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3899125 143641 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
44627123 6047 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1080490 6047 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
44627025 6362 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1082106 6362 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
23630606 92260 None 0 Human Functional pKi = 9.4 9.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cc1 10.1021/jm0705612
CHEMBL242600 92260 None 0 Human Functional pKi = 9.4 9.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cc1 10.1021/jm0705612
44626929 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1079481 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
44627133 6331 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1081957 6331 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
44626929 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.07.073
CHEMBL1079481 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.07.073
44626929 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079481 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
11305766 5915 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 462 7 0 6 5.2 Cc1ccoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079639 5915 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 462 7 0 6 5.2 Cc1ccoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
44627357 5993 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080126 5993 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
44627133 6331 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081957 6331 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
44626929 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm100832d
CHEMBL1079481 5886 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm100832d
121304538 150093 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
CHEMBL3950254 150093 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
121304551 151721 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 427 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3963783 151721 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 427 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121315401 153197 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 478 7 0 6 5.9 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccs1 10.1021/acs.jmedchem.6b00972
CHEMBL3976319 153197 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 478 7 0 6 5.9 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccs1 10.1021/acs.jmedchem.6b00972
121304441 152473 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 152473 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
121304649 150733 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3955505 150733 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
11996304 15213 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210614 15213 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
45267491 198448 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 3 4.1 O=C1N(CCN2CCCc3sccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL559873 198448 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 3 4.1 O=C1N(CCN2CCCc3sccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
11260032 5885 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 474 7 0 7 4.4 Cc1cnc(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)cn1 10.1021/jm901319p
CHEMBL1079480 5885 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 474 7 0 7 4.4 Cc1cnc(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)cn1 10.1021/jm901319p
44627357 5993 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080126 5993 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
44626744 6277 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 458 7 0 5 5.3 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccccc1 10.1021/jm901319p
CHEMBL1081686 6277 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 458 7 0 5 5.3 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccccc1 10.1021/jm901319p
44627359 6317 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081868 6317 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1204409 6317 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
46931815 17310 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 479 7 0 7 6.0 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(C)(C)C)cc2)C3)n1C 10.1021/jm100832d
CHEMBL1257215 17310 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 479 7 0 7 6.0 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(C)(C)C)cc2)C3)n1C 10.1021/jm100832d
9828617 92996 None 5 Human Functional pKi = 9.2 9.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 536 7 1 7 4.2 Cc1nc(-c2cccc(C(=O)N[C@H]3CC[C@H](CCN4CCc5ccc(S(C)(=O)=O)cc5CC4)CC3)c2)no1 10.1021/jm0705612
CHEMBL244083 92996 None 5 Human Functional pKi = 9.2 9.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 536 7 1 7 4.2 Cc1nc(-c2cccc(C(=O)N[C@H]3CC[C@H](CCN4CCc5ccc(S(C)(=O)=O)cc5CC4)CC3)c2)no1 10.1021/jm0705612
CHEMBL3084616 92996 None 5 Human Functional pKi = 9.2 9.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 536 7 1 7 4.2 Cc1nc(-c2cccc(C(=O)N[C@H]3CC[C@H](CCN4CCc5ccc(S(C)(=O)=O)cc5CC4)CC3)c2)no1 10.1021/jm0705612
23631454 93161 None 0 Human Functional pKi = 9.2 9.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(Cl)cc4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244279 93161 None 0 Human Functional pKi = 9.2 9.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(Cl)cc4)n2C)CC3)no1 10.1021/jm0705612
121304654 148965 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3941520 148965 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304485 148263 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3935692 148263 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
11996303 15207 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210552 15207 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
11699532 155249 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 542 7 0 9 5.2 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL402215 155249 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 542 7 0 9 5.2 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
11504077 168932 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL437792 168932 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
44627127 5881 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1079461 5881 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
11477018 5916 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 6 5.0 Cc1ccc(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)cn1 10.1021/jm901319p
CHEMBL1079640 5916 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 6 5.0 Cc1ccc(-c2nnc(SCCCN3C[C@@H]4C[C@]4(c4ccc(C(F)(F)F)cc4)C3)n2C)cn1 10.1021/jm901319p
44627023 5945 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079822 5945 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
44627355 5968 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
CHEMBL1079938 5968 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
44626928 6017 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(F)(F)F)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1080293 6017 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(F)(F)F)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627359 6317 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081868 6317 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1204409 6317 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
11720838 167281 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 6 0 8 6.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL429132 167281 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 6 0 8 6.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
121315244 149673 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 473 7 0 6 5.3 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccccn1 10.1021/acs.jmedchem.6b00972
CHEMBL3946901 149673 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 473 7 0 6 5.3 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccccn1 10.1021/acs.jmedchem.6b00972
44249745 197899 None 1 Rat Functional pKi = 9.1 9.1 - 0
Antagonistic activity at rat DRD3 receptorAntagonistic activity at rat DRD3 receptor
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.07.055
CHEMBL552373 197899 None 1 Rat Functional pKi = 9.1 9.1 - 0
Antagonistic activity at rat DRD3 receptorAntagonistic activity at rat DRD3 receptor
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.07.055
CHEMBL567286 197899 None 1 Rat Functional pKi = 9.1 9.1 - 0
Antagonistic activity at rat DRD3 receptorAntagonistic activity at rat DRD3 receptor
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.07.055
23631173 92259 None 0 Human Functional pKi = 9.1 9.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1cccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)c1 10.1021/jm0705612
CHEMBL242599 92259 None 0 Human Functional pKi = 9.1 9.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1cccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)c1 10.1021/jm0705612
23631091 150972 None 0 Human Functional pKi = 9.1 9.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 462 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccn4C)n2C)CC3)no1 10.1021/jm0705612
CHEMBL395743 150972 None 0 Human Functional pKi = 9.1 9.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 462 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccn4C)n2C)CC3)no1 10.1021/jm0705612
11996303 15207 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210552 15207 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
11621352 97686 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL271034 97686 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
44626740 5992 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1080117 5992 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627120 6046 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
CHEMBL1080489 6046 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
44627242 6120 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080846 6120 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
11225043 6226 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081409 6226 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
11751828 6278 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 6 5.0 Cc1ncccc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081687 6278 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 6 5.0 Cc1ncccc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
11397017 6316 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 460 7 0 7 4.0 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccnnc1 10.1021/jm901319p
CHEMBL1081867 6316 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 460 7 0 7 4.0 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccnnc1 10.1021/jm901319p
44626530 6329 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081934 6329 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
44627240 6332 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081966 6332 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
11606176 95187 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 527 7 0 9 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(N(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255620 95187 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 527 7 0 9 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(N(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882051 6240 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 355 4 0 2 3.8 O=C1N(CCN2CCCCCC2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081488 6240 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 355 4 0 2 3.8 O=C1N(CCN2CCCCCC2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.01.090
44249745 197899 None 1 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL552373 197899 None 1 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL567286 197899 None 1 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
45269020 198524 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 467 4 0 2 3.8 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(I)c1 10.1016/j.bmcl.2009.06.028
CHEMBL560574 198524 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 467 4 0 2 3.8 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(I)c1 10.1016/j.bmcl.2009.06.028
23630903 150968 None 0 Human Functional pKi = 9 9.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2cc(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)on6)cc5CC4)n3C)ccc2n1 10.1021/jm0705612
CHEMBL395741 150968 None 0 Human Functional pKi = 9 9.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2cc(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)on6)cc5CC4)n3C)ccc2n1 10.1021/jm0705612
23630501 152718 None 0 Human Functional pKi = 9 9.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 527 7 0 7 6.3 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(Cl)c(Cl)c4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL397222 152718 None 0 Human Functional pKi = 9 9.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 527 7 0 7 6.3 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(Cl)c(Cl)c4)n2C)CC3)no1 10.1021/jm0705612
11584660 93321 None 8 Human Functional pKi = 9 9.0 - 5
Displacement of [35S]GTP-gamma-S from human recombinant dopamine D3 receptor expressed in CHO cells after 30 mins at 10 uMDisplacement of [35S]GTP-gamma-S from human recombinant dopamine D3 receptor expressed in CHO cells after 30 mins at 10 uM
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 93321 None 8 Human Functional pKi = 9 9.0 - 5
Displacement of [35S]GTP-gamma-S from human recombinant dopamine D3 receptor expressed in CHO cells after 30 mins at 10 uMDisplacement of [35S]GTP-gamma-S from human recombinant dopamine D3 receptor expressed in CHO cells after 30 mins at 10 uM
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
121304711 150025 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 491 7 0 6 5.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)nnc1-c1cccnc1 10.1021/acs.jmedchem.6b00972
CHEMBL3949662 150025 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 491 7 0 6 5.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)nnc1-c1cccnc1 10.1021/acs.jmedchem.6b00972
11996304 15213 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210614 15213 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
16123247 16295 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 386 6 2 4 3.5 COc1cc([C@]23CNC[C@H]2C3)ccc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1224699 16295 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 386 6 2 4 3.5 COc1cc([C@]23CNC[C@H]2C3)ccc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/j.bmcl.2010.07.073
45273522 198978 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 333 4 0 2 3.6 O=C1N(CCN2[C@H]3CCC[C@@H]2CC3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL563580 198978 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 333 4 0 2 3.6 O=C1N(CCN2[C@H]3CCC[C@@H]2CC3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
44626738 5904 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079578 5904 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
44627355 5968 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
CHEMBL1079938 5968 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
44626835 6001 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 533 7 0 6 5.9 Cc1ccc2c(-c3nnc(SCCCN4C[C@@H]5C[C@]5(c5ccc(Br)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1080165 6001 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 533 7 0 6 5.9 Cc1ccc2c(-c3nnc(SCCCN4C[C@@H]5C[C@]5(c5ccc(Br)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627123 6047 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1080490 6047 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
24743758 6152 None 20 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081023 6152 None 20 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
44627470 6225 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 8 0 8 4.6 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1C(F)(F)F 10.1021/jm901319p
CHEMBL1081408 6225 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 8 0 8 4.6 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1C(F)(F)F 10.1021/jm901319p
44627351 6257 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081587 6257 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
45268112 198666 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.3 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL561512 198666 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.3 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.06.028
45271511 199924 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 357 4 1 3 2.9 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL569846 199924 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 357 4 1 3 2.9 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(O)c1 10.1016/j.bmcl.2009.06.028
23631172 92258 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 467 7 0 8 4.3 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCOCC4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL242598 92258 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 467 7 0 8 4.3 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCOCC4)n2C)CC3)no1 10.1021/jm0705612
23630602 92901 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 479 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCC(C)CC4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243860 92901 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 479 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCC(C)CC4)n2C)CC3)no1 10.1021/jm0705612
23630497 92999 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 465 7 0 8 5.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccs4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244086 92999 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 465 7 0 8 5.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccs4)n2C)CC3)no1 10.1021/jm0705612
135846033 152952 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 498 7 1 7 5.5 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cc5ccccc5[nH]4)n2C)CC3)o1 10.1021/jm0705612
CHEMBL397429 152952 None 0 Human Functional pKi = 8.9 8.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 498 7 1 7 5.5 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cc5ccccc5[nH]4)n2C)CC3)o1 10.1021/jm0705612
9904074 110691 None 3 Human Functional pKi = 8.9 8.9 - 1
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1016/j.ejmech.2022.114378
CHEMBL325710 110691 None 3 Human Functional pKi = 8.9 8.9 - 1
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1016/j.ejmech.2022.114378
121304464 144432 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
CHEMBL3905582 144432 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
121304597 146512 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 441 7 0 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(F)cc3F)C2)nnc1-c1cccnc1 10.1021/acs.jmedchem.6b00972
CHEMBL3921885 146512 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 441 7 0 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(F)cc3F)C2)nnc1-c1cccnc1 10.1021/acs.jmedchem.6b00972
121304500 149842 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
CHEMBL3948167 149842 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
11584660 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL244946 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11691697 97769 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 492 6 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL271449 97769 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 492 6 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
11584660 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
CHEMBL244946 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
45272635 198263 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 423 6 0 2 5.1 CN(CCN1CCN(c2cccc(C(F)(F)F)c2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
CHEMBL558058 198263 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 423 6 0 2 5.1 CN(CCN1CCN(c2cccc(C(F)(F)F)c2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
11775544 5883 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 460 7 0 7 4.0 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cncnc1 10.1021/jm901319p
CHEMBL1079475 5883 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 460 7 0 7 4.0 Cn1c(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cncnc1 10.1021/jm901319p
24743758 6152 None 20 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081023 6152 None 20 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
44626637 6224 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081401 6224 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44626530 6329 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081934 6329 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
44627353 6364 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
CHEMBL1082111 6364 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
11584660 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL244946 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm901319p
44454190 98118 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1 10.1016/j.bmcl.2007.12.066
CHEMBL273199 98118 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 537 7 0 8 5.6 Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1 10.1016/j.bmcl.2007.12.066
46882007 6215 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 355 4 0 2 4.1 O=C1N(CCN2CCCCCC2)CCN1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081309 6215 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 355 4 0 2 4.1 O=C1N(CCN2CCCCCC2)CCN1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2010.01.090
45273266 198084 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL556272 198084 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.028
45273292 198833 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 3.9 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL562624 198833 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 3.9 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
45268113 199183 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 391 5 0 3 3.8 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
CHEMBL565017 199183 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 391 5 0 3 3.8 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
11663999 92263 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 551 7 0 8 6.0 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL242603 92263 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 551 7 0 8 6.0 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
23630999 92871 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 459 7 0 7 5.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccc4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243709 92871 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 459 7 0 7 5.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccc4)n2C)CC3)no1 10.1021/jm0705612
23630900 93158 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 498 7 1 7 5.5 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc5[nH]ccc5c4)n2C)CC3)o1 10.1021/jm0705612
CHEMBL244276 93158 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 498 7 1 7 5.5 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc5[nH]ccc5c4)n2C)CC3)o1 10.1021/jm0705612
23630901 93159 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 462 7 0 8 4.4 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccn4C)n2C)CC3)o1 10.1021/jm0705612
CHEMBL244277 93159 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 462 7 0 8 4.4 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccn4C)n2C)CC3)o1 10.1021/jm0705612
23631092 93160 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccc(Cl)c4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244278 93160 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccc(Cl)c4)n2C)CC3)no1 10.1021/jm0705612
44428207 93162 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 477 7 0 7 5.2 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccc(F)c4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244280 93162 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 477 7 0 7 5.2 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccc(F)c4)n2C)CC3)no1 10.1021/jm0705612
11584660 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 93321 None 8 Human Functional pKi = 8.8 8.8 - 5
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
11555265 93347 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 508 7 0 7 5.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(F)c(F)c4)n2C)CC3)n(C)n1 10.1021/jm0705612
CHEMBL245118 93347 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 508 7 0 7 5.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(F)c(F)c4)n2C)CC3)n(C)n1 10.1021/jm0705612
23631366 150970 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 473 7 0 7 5.3 Cc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cc1 10.1021/jm0705612
CHEMBL395742 150970 None 0 Human Functional pKi = 8.8 8.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 473 7 0 7 5.3 Cc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cc1 10.1021/jm0705612
11548239 95352 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 528 7 0 8 6.1 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL256442 95352 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 528 7 0 8 6.1 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
11606378 95368 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL256488 95368 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
44627033 5950 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079837 5950 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
44626637 6224 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081401 6224 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627240 6332 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081966 6332 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
44627025 6362 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1082106 6362 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
11705929 92262 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 494 6 0 7 4.7 Cc1cc(-c2ccc3c(c2)CCN(CCSc2nnc(-c4ccc(F)c(F)c4)n2C)CC3)n(C)n1 10.1021/jm0705612
CHEMBL242602 92262 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 494 6 0 7 4.7 Cc1cc(-c2ccc3c(c2)CCN(CCSc2nnc(-c4ccc(F)c(F)c4)n2C)CC3)n(C)n1 10.1021/jm0705612
23630902 92869 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)on6)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL243707 92869 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)on6)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
23631540 92900 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 451 7 0 7 5.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCCC4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243859 92900 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 451 7 0 7 5.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C4CCCC4)n2C)CC3)no1 10.1021/jm0705612
23630796 92997 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6ncc(C)o6)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244084 92997 None 0 Human Functional pKi = 8.7 8.7 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6ncc(C)o6)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
45273551 198886 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 355 6 0 2 4.1 CN(CCN1CCN(c2ccccc2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
CHEMBL562948 198886 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 355 6 0 2 4.1 CN(CCN1CCN(c2ccccc2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
44627466 6318 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 427 7 0 7 4.0 Cc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c(F)c1 10.1021/jm901319p
CHEMBL1081869 6318 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 427 7 0 7 4.0 Cc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c(F)c1 10.1021/jm901319p
49781476 17342 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.7 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(F)(F)F)cc2)C3)n1C 10.1021/jm100832d
CHEMBL1257336 17342 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.7 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(F)(F)F)cc2)C3)n1C 10.1021/jm100832d
52940788 17528 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 505 7 0 7 5.6 Cc1nc(C)c(-c2nnc(SCCCN3CCC4CC4(c4ccc(C(F)(F)F)cc4)CC3)n2C)o1 10.1021/jm100832d
CHEMBL1257925 17528 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 505 7 0 7 5.6 Cc1nc(C)c(-c2nnc(SCCCN3CCC4CC4(c4ccc(C(F)(F)F)cc4)CC3)n2C)o1 10.1021/jm100832d
11590828 95270 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 466 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(C)C)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL256016 95270 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 466 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(C)C)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
121304685 145473 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 493 7 1 6 4.2 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCNC(=O)C1 10.1021/acs.jmedchem.6b00972
CHEMBL3913849 145473 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 493 7 1 6 4.2 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCNC(=O)C1 10.1021/acs.jmedchem.6b00972
121304754 154052 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 507 7 0 6 4.5 CN1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1=O 10.1021/acs.jmedchem.6b00972
CHEMBL3983684 154052 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 507 7 0 6 4.5 CN1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1=O 10.1021/acs.jmedchem.6b00972
45268142 198451 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 371 5 0 3 3.2 COc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL559920 198451 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 371 5 0 3 3.2 COc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
23631458 92910 None 0 Human Functional pKi = 8 8.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 451 6 0 7 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(F)(F)F)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243900 92910 None 0 Human Functional pKi = 8 8.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 451 6 0 7 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(F)(F)F)n2C)CC3)no1 10.1021/jm0705612
23630505 92911 None 0 Human Functional pKi = 8 8.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 425 7 0 7 4.5 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(C)C)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243901 92911 None 0 Human Functional pKi = 8 8.0 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 425 7 0 7 4.5 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(C)C)n2C)CC3)no1 10.1021/jm0705612
46882520 5858 None 0 Human Functional pKi = 7 7.0 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5858 None 0 Human Functional pKi = 7 7.0 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
44454358 155280 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL402422 155280 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
45273529 198179 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 413 7 0 3 4.3 O=C1N(CCN2CCCC(OCc3ccccc3)C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL557110 198179 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 413 7 0 3 4.3 O=C1N(CCN2CCCC(OCc3ccccc3)C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
24815439 204392 None 1 Human Functional pKi = 7 7.0 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 323 3 0 3 4.1 Cn1c(CN2CCC(c3ccccc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL607689 204392 None 1 Human Functional pKi = 7 7.0 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 323 3 0 3 4.1 Cn1c(CN2CCC(c3ccccc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
44627245 5944 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 477 7 0 7 4.9 Cc1cc(C(F)(F)F)ccc1C12CC1CN(CCCSc1nnc(-c3ocnc3C)n1C)C2 10.1021/jm901319p
CHEMBL1079814 5944 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 477 7 0 7 4.9 Cc1cc(C(F)(F)F)ccc1C12CC1CN(CCCSc1nnc(-c3ocnc3C)n1C)C2 10.1021/jm901319p
44627033 5950 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079837 5950 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
24758834 17695 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1ccc2c(c1)CCCC21CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
CHEMBL1258492 17695 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1ccc2c(c1)CCCC21CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
24758838 17732 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 425 6 0 8 3.7 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCOc4ccccc43)C2)n1C 10.1021/jm100832d
CHEMBL1258606 17732 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 425 6 0 8 3.7 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCOc4ccccc43)C2)n1C 10.1021/jm100832d
11578028 95149 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 604 7 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(C(C)CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL255417 95149 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 604 7 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(C(C)CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11534726 95185 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 644 6 0 8 7.2 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255618 95185 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 644 6 0 8 7.2 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11662194 97530 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 441 6 0 8 3.7 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(C2CCOCC2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL270209 97530 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 441 6 0 8 3.7 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(C2CCOCC2)n1C)CC3 10.1016/j.bmcl.2007.12.066
11712044 97929 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 448 7 0 8 4.2 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccnc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272302 97929 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 448 7 0 8 4.2 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccnc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
45268120 199091 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 2 4.2 CC(C)(C)c1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)cc1 10.1016/j.bmcl.2009.06.028
CHEMBL564298 199091 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 2 4.2 CC(C)(C)c1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)cc1 10.1016/j.bmcl.2009.06.028
11996303 15207 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210552 15207 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(S(F)(F)(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2010.06.018
11705119 166579 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 452 7 0 9 4.1 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL427836 166579 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 452 7 0 9 4.1 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
45271737 198974 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 2 4.5 CC1(C)C[C@@H]2C[C@@](C)(CN2CCN2CCN(c3cccc(Cl)c3)C2=O)C1 10.1016/j.bmcl.2009.06.043
CHEMBL563563 198974 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 2 4.5 CC1(C)C[C@@H]2C[C@@](C)(CN2CCN2CCN(c3cccc(Cl)c3)C2=O)C1 10.1016/j.bmcl.2009.06.043
44627127 5881 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1079461 5881 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
44627022 5922 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 395 7 0 7 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccccc3)C2)n1C 10.1021/jm901319p
CHEMBL1079667 5922 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 395 7 0 7 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccccc3)C2)n1C 10.1021/jm901319p
44626734 6194 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081237 6194 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
52947516 17458 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm100832d
CHEMBL1257687 17458 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm100832d
44454458 95178 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 618 6 0 8 7.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255566 95178 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 618 6 0 8 7.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11519858 97946 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 578 7 0 9 4.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(S(C)(=O)=O)CCO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272379 97946 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 578 7 0 9 4.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(S(C)(=O)=O)CCO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11519134 97984 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272545 97984 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11685267 98112 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 538 8 0 8 6.0 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(CC7CC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL273166 98112 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 538 8 0 8 6.0 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(CC7CC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11518972 155122 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 501 6 0 7 5.5 Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL401576 155122 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 501 6 0 7 5.5 Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
45271491 197636 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.3 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL550502 197636 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.3 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.06.028
45272414 197895 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.0 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
CHEMBL552366 197895 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.0 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
11598123 93348 None 0 Human Functional pKi = 7.9 7.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 477 7 0 9 4.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ocnc4C)n2C)CC3)n(C)n1 10.1021/jm0705612
CHEMBL245119 93348 None 0 Human Functional pKi = 7.9 7.9 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 477 7 0 9 4.1 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ocnc4C)n2C)CC3)n(C)n1 10.1021/jm0705612
45270916 197289 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 348 6 0 4 3.0 Cc1cc(CN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)on1 10.1016/j.bmcl.2009.06.043
CHEMBL549438 197289 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 348 6 0 4 3.0 Cc1cc(CN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)on1 10.1016/j.bmcl.2009.06.043
45271753 198010 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 417 9 0 4 3.8 COc1ccc(CCN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)cc1OC 10.1016/j.bmcl.2009.06.043
CHEMBL554693 198010 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 417 9 0 4 3.8 COc1ccc(CCN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)cc1OC 10.1016/j.bmcl.2009.06.043
45273530 199034 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 387 8 0 3 3.8 COc1cccc(CCN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)c1 10.1016/j.bmcl.2009.06.043
CHEMBL563926 199034 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 387 8 0 3 3.8 COc1cccc(CCN(C)CCN2CCN(c3cccc(Cl)c3)C2=O)c1 10.1016/j.bmcl.2009.06.043
24815434 202152 None 0 Human Functional pKi = 6.9 6.9 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593196 202152 None 0 Human Functional pKi = 6.9 6.9 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24743758 6152 None 20 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081023 6152 None 20 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm901319p
44627353 6364 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
CHEMBL1082111 6364 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
52948653 17377 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 7 0 7 3.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccccc3)C2)n1C 10.1021/jm100832d
CHEMBL1257447 17377 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 7 0 7 3.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccccc3)C2)n1C 10.1021/jm100832d
49780809 17558 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
CHEMBL1258035 17558 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
44454371 95401 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 434 6 0 8 3.9 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccnc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256653 95401 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 434 6 0 8 3.9 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccnc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454166 95590 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 7 0 8 6.3 CCc1nc2cc3c(c(C)c2o1)CCN(C(C)CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL257524 95590 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 7 0 8 6.3 CCc1nc2cc3c(c(C)c2o1)CCN(C(C)CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454217 95679 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 552 5 0 8 6.0 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257900 95679 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 552 5 0 8 6.0 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454339 97889 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 7 0 7 5.7 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272086 97889 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 7 0 7 5.7 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882049 5608 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1ccc(N2CCN(CCN3CCCCCC3)C2=O)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1077348 5608 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1ccc(N2CCN(CCN3CCCCCC3)C2=O)cc1 10.1016/j.bmcl.2010.01.090
46881413 7383 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 333 5 0 4 3.6 O=c1n(CCCN2CCCCCC2)ccn1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1086395 7383 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 333 5 0 4 3.6 O=c1n(CCCN2CCCCCC2)ccn1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
45269000 198349 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 347 4 0 3 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc2occc2c1 10.1016/j.bmcl.2009.06.028
CHEMBL559004 198349 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 347 4 0 3 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc2occc2c1 10.1016/j.bmcl.2009.06.028
45273273 198925 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 3 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1c1csc2ccccc12 10.1016/j.bmcl.2009.06.028
CHEMBL563247 198925 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 3 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1c1csc2ccccc12 10.1016/j.bmcl.2009.06.028
45273293 199063 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 5 0 4 2.0 CC(C)N1CCN(CCN2CCN(c3ccc(F)c(C#N)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL564108 199063 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 5 0 4 2.0 CC(C)N1CCN(CCN2CCN(c3ccc(F)c(C#N)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
45271499 200150 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL571229 200150 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
11996304 15213 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
CHEMBL1210614 15213 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assayAntagonist activity at dopamine D3 receptor assessed as inhibition of dopamine-induced [35S]GTPgammaS binding by FLIPR assay
ChEMBL 521 8 0 7 6.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(S(F)(F)(F)(F)F)c3)C2)n1C 10.1016/j.bmcl.2010.06.018
11533448 95105 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 502 6 0 8 4.9 Cc1ncccc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL255158 95105 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 502 6 0 8 4.9 Cc1ncccc1-c1nnc(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
45272616 199171 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 2 4.3 CC1(C)[C@H]2CC[C@]1(C)CN(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
CHEMBL564930 199171 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 375 4 0 2 4.3 CC1(C)[C@H]2CC[C@]1(C)CN(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
44627133 6331 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081957 6331 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
24758830 17658 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 501 6 0 7 5.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCCc4ccc(Br)cc43)C2)n1C 10.1021/jm100832d
CHEMBL1258381 17658 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 501 6 0 7 5.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCCc4ccc(Br)cc43)C2)n1C 10.1021/jm100832d
46882053 6242 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081490 6242 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
45268987 198761 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 350 4 0 3 3.0 N#Cc1cc(N2CCN(CCN3Cc4ccccc4C3)C2=O)ccc1F 10.1016/j.bmcl.2009.06.028
CHEMBL562176 198761 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 350 4 0 3 3.0 N#Cc1cc(N2CCN(CCN3Cc4ccccc4C3)C2=O)ccc1F 10.1016/j.bmcl.2009.06.028
11678080 93349 None 0 Human Functional pKi = 7.8 7.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 523 6 0 8 5.2 Cc1ccc2c(-c3nnc(SCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL245120 93349 None 0 Human Functional pKi = 7.8 7.8 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 523 6 0 8 5.2 Cc1ccc2c(-c3nnc(SCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
44454384 95636 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 497 6 0 8 4.9 Cc1ccn2c3c(nc2c1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL257717 95636 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 497 6 0 8 4.9 Cc1ccn2c3c(nc2c1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
44454320 97822 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(C(F)(F)F)cn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL271729 97822 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(C(F)(F)F)cn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
45268333 195965 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 377 6 0 3 3.2 COCC1[C@@H]2CC[C@H]1CN(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
CHEMBL541435 195965 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 377 6 0 3 3.2 COCC1[C@@H]2CC[C@H]1CN(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
45268346 198628 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 5 4.5 O=C1N(CCN2CCC(c3nnc(-c4ccccc4)o3)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL561326 198628 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 5 4.5 O=C1N(CCN2CCC(c3nnc(-c4ccccc4)o3)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
44626734 6194 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081237 6194 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
52947507 17417 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 7 0 7 3.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4ccccc4)CC3C2)n1C 10.1021/jm100832d
CHEMBL1257565 17417 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 7 0 7 3.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4ccccc4)CC3C2)n1C 10.1021/jm100832d
52946432 17836 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 427 6 0 7 4.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4cc(F)ccc43)C2)n1C 10.1021/jm100832d
CHEMBL1258949 17836 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 427 6 0 7 4.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4cc(F)ccc43)C2)n1C 10.1021/jm100832d
44454120 95225 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL255827 95225 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454168 95364 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4onc(C)c4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL256475 95364 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 6 0 9 3.8 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4onc(C)c4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
44454223 98027 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 542 6 0 8 4.7 CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272702 98027 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 542 6 0 8 4.7 CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
45272437 197618 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 346 6 0 4 2.0 COc1cccc(N2CCN(CCN3CCN(C(C)C)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL550358 197618 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 346 6 0 4 2.0 COc1cccc(N2CCN(CCN3CCN(C(C)C)CC3)C2=O)c1 10.1016/j.bmcl.2009.06.028
45272415 197896 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2009.06.028
CHEMBL552367 197896 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2009.06.028
45267262 197947 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.028
CHEMBL553238 197947 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.028
45272435 200119 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 368 5 0 3 2.7 CC(C)N1CCN(CCN2CCN(c3cccc(Cl)c3F)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL570998 200119 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 368 5 0 3 2.7 CC(C)N1CCN(CCN2CCN(c3cccc(Cl)c3F)C2=O)CC1 10.1016/j.bmcl.2009.06.028
45272438 200149 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 322 4 0 3 1.8 CN1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL571221 200149 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 322 4 0 3 1.8 CN1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
46225584 202131 None 0 Human Functional pKi = 5.8 5.8 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593056 202131 None 0 Human Functional pKi = 5.8 5.8 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225581 204444 None 0 Human Functional pKi = 5.8 5.8 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL608103 204444 None 0 Human Functional pKi = 5.8 5.8 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
154706123 176393 None 1 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assayAntagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 176393 None 1 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assayAntagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 176393 None 1 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assayAntagonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as suppression of dopamine-induced inhibition of isoproterenol-stimulated cAMP accumulation preincubated for 10 mins followed by dopamine stimulation and measured after 20 mins by Glosensor-based luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
46882522 5714 None 0 Human Functional pKi = 7.7 7.7 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5714 None 0 Human Functional pKi = 7.7 7.7 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
11540474 95402 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 492 6 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4nc(C(F)(F)F)oc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL256659 95402 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 492 6 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4nc(C(F)(F)F)oc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
45271738 197831 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 0 2 5.2 C[C@@]12CC(c3ccccc3)C[C@@H](C1)N(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
CHEMBL551927 197831 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 0 2 5.2 C[C@@]12CC(c3ccccc3)C[C@@H](C1)N(CCN1CCN(c3cccc(Cl)c3)C1=O)C2 10.1016/j.bmcl.2009.06.043
45267504 198488 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 369 6 0 2 4.4 Cc1cccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)c1 10.1016/j.bmcl.2009.06.043
CHEMBL560270 198488 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 369 6 0 2 4.4 Cc1cccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)c1 10.1016/j.bmcl.2009.06.043
44626637 6224 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081401 6224 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 511 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C(C)(C)C)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
11562200 95363 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(C)(F)F)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL256474 95363 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(C)(F)F)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
11657494 95562 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 644 7 0 8 7.2 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257369 95562 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 644 7 0 8 7.2 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11648990 95699 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257946 95699 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11663526 97805 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271632 97805 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
45267251 198889 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL562983 198889 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2009.06.028
45102707 5759 None 0 Human Functional pKi = 6.7 6.7 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
CHEMBL1078492 5759 None 0 Human Functional pKi = 6.7 6.7 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
49865623 16038 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc(C34CNCC3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223657 16038 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc(C34CNCC3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
44454352 97998 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 491 6 0 9 4.0 Cc1ncoc1-c1nnc(SCCCN2CCc3nc4cc(C(F)(F)F)ccn4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL272588 97998 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 491 6 0 9 4.0 Cc1ncoc1-c1nnc(SCCCN2CCc3nc4cc(C(F)(F)F)ccn4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
44626527 5889 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
CHEMBL1079494 5889 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
44627357 5993 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080126 5993 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(C(F)(F)F)c(F)c3)C2)n1C 10.1021/jm901319p
44627470 6225 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 8 0 8 4.6 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1C(F)(F)F 10.1021/jm901319p
CHEMBL1081408 6225 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 493 8 0 8 4.6 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1C(F)(F)F 10.1021/jm901319p
44454118 95188 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 424 6 0 9 3.5 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4ncoc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL255621 95188 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 424 6 0 9 3.5 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4ncoc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
44454403 97738 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 464 7 0 9 4.4 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C5CC5)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL271280 97738 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 464 7 0 9 4.4 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C5CC5)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
44454248 97945 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 576 6 0 8 6.0 CCc1nc2cc3c(c(Br)c2o1)CCN(CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272378 97945 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 576 6 0 8 6.0 CCc1nc2cc3c(c(Br)c2o1)CCN(CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
45270678 197913 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 327 4 0 3 3.3 Cc1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)s1 10.1016/j.bmcl.2009.06.028
CHEMBL552460 197913 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 327 4 0 3 3.3 Cc1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)s1 10.1016/j.bmcl.2009.06.028
45273278 198154 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 390 5 0 4 4.1 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cscc1-c1ccccn1 10.1016/j.bmcl.2009.06.028
CHEMBL556895 198154 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 390 5 0 4 4.1 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cscc1-c1ccccn1 10.1016/j.bmcl.2009.06.028
121304417 144219 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 506 7 0 6 5.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CC2CCC(C1)O2 10.1021/acs.jmedchem.6b00972
CHEMBL3903779 144219 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 506 7 0 6 5.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CC2CCC(C1)O2 10.1021/acs.jmedchem.6b00972
16123136 16283 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1224638 16283 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
16123138 16294 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 396 7 1 3 4.4 C=CCN1C[C@H]2C[C@@]2(c2ccc(NS(=O)(=O)c3ccc(C(C)C)cc3)cc2)C1 10.1016/j.bmcl.2010.07.073
CHEMBL1224698 16294 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 396 7 1 3 4.4 C=CCN1C[C@H]2C[C@@]2(c2ccc(NS(=O)(=O)c3ccc(C(C)C)cc3)cc2)C1 10.1016/j.bmcl.2010.07.073
11562199 98044 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4nc(C(C)(F)F)oc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL272775 98044 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4nc(C(C)(F)F)oc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
44517726 198478 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL560177 198478 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
45267480 198804 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 409 4 0 2 4.5 O=C1N(CCN2C[C@@H]3CC[C@H]2Cc2ccccc2C3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL562464 198804 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 409 4 0 2 4.5 O=C1N(CCN2C[C@@H]3CC[C@H]2Cc2ccccc2C3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
45268438 198985 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 295 6 0 2 2.9 CCN(CC)CCN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.043
CHEMBL563635 198985 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 295 6 0 2 2.9 CCN(CC)CCN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.043
45267471 199021 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 319 4 0 2 3.1 O=C1N(CCN2C[C@H]3CC[C@@H]2C3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL563860 199021 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 319 4 0 2 3.1 O=C1N(CCN2C[C@H]3CC[C@@H]2C3)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
44627468 6291 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081747 6291 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
24758715 17805 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4ccc(Br)cc43)C2)n1C 10.1021/jm100832d
CHEMBL1258833 17805 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4ccc(Br)cc43)C2)n1C 10.1021/jm100832d
11569996 95365 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 525 7 0 8 5.4 CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256477 95365 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 525 7 0 8 5.4 CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11497411 97804 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 7 0 8 6.1 CCc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL271631 97804 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 7 0 8 6.1 CCc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
45271510 197827 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.3 CC1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL551914 197827 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.3 CC1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
45271548 198350 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.0 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
CHEMBL559029 198350 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 375 4 0 2 4.0 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
45267254 198444 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 332 4 0 3 2.8 N#Cc1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL559856 198444 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 332 4 0 3 2.8 N#Cc1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
44517726 198478 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL560177 198478 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.028
23631001 92908 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 460 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccn4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243898 92908 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 460 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccn4)n2C)CC3)no1 10.1021/jm0705612
23630499 93000 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccc4Cl)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244087 93000 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 493 7 0 7 5.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccccc4Cl)n2C)CC3)no1 10.1021/jm0705612
23631544 93320 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 490 8 0 9 4.4 COc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cn1 10.1021/jm0705612
CHEMBL244945 93320 None 0 Human Functional pKi = 8.6 8.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 490 8 0 9 4.4 COc1ccc(-c2nnc(SCCCN3CCc4ccc(-c5cc(C)on5)cc4CC3)n2C)cn1 10.1021/jm0705612
134150637 151654 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3963243 151654 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
121315197 144820 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 491 8 0 7 5.5 Cc1ncoc1-c1nnc(SCCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3908862 144820 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 491 8 0 7 5.5 Cc1ncoc1-c1nnc(SCCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
16123347 16022 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 355 5 1 3 3.6 CC(C)c1ccc(S(=O)(=O)Cc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223598 16022 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 355 5 1 3 3.6 CC(C)c1ccc(S(=O)(=O)Cc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
16123467 16024 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 355 5 1 3 3.6 CC(C)c1ccc(CS(=O)(=O)c2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223600 16024 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 355 5 1 3 3.6 CC(C)c1ccc(CS(=O)(=O)c2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
11663578 97928 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 518 7 0 11 4.2 Cc1cc(-c2nc3c4c(ccc3o2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)CC4)n(C)n1 10.1016/j.bmcl.2007.12.042
CHEMBL272297 97928 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 518 7 0 11 4.2 Cc1cc(-c2nc3c4c(ccc3o2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)CC4)n(C)n1 10.1016/j.bmcl.2007.12.042
45267492 198863 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 387 4 0 2 4.5 CC1(C)[C@@H]2CC[C@]13CCN(CCN1CCN(c4cccc(Cl)c4)C1=O)C3C2 10.1016/j.bmcl.2009.06.043
CHEMBL562833 198863 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 387 4 0 2 4.5 CC1(C)[C@@H]2CC[C@]13CCN(CCN1CCN(c4cccc(Cl)c4)C1=O)C3C2 10.1016/j.bmcl.2009.06.043
45267503 199174 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 369 6 0 2 4.4 Cc1ccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)cc1 10.1016/j.bmcl.2009.06.043
CHEMBL564948 199174 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 369 6 0 2 4.4 Cc1ccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)cc1 10.1016/j.bmcl.2009.06.043
44627242 6120 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080846 6120 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
44626632 6188 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 455 7 0 6 5.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccccc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081203 6188 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 455 7 0 6 5.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccccc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627359 6317 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081868 6317 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1204409 6317 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(F)cc(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
11585034 95221 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 576 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255806 95221 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 576 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11562113 95399 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 483 7 0 7 5.0 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(F)c(F)c2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256651 95399 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 483 7 0 7 5.0 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(F)c(F)c2)n1C)CC3 10.1016/j.bmcl.2007.12.066
11692376 97487 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 8 0 8 6.3 CCc1nc2cc3c(c(C)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL269994 97487 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 8 0 8 6.3 CCc1nc2cc3c(c(C)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11620847 97958 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 7 0 7 5.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272478 97958 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 540 7 0 7 5.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11591601 155423 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL403181 155423 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11533429 169082 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 501 6 0 7 5.5 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL439065 169082 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 501 6 0 7 5.5 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
46881408 6760 None 0 Human Functional pKi = 7.6 7.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 339 4 0 2 3.6 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1083813 6760 None 0 Human Functional pKi = 7.6 7.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 339 4 0 2 3.6 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.01.090
23631368 92998 None 0 Human Functional pKi = 7.6 7.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 460 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccncc4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL244085 92998 None 0 Human Functional pKi = 7.6 7.6 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 460 7 0 8 4.4 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccncc4)n2C)CC3)no1 10.1021/jm0705612
16123349 16296 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 382 4 2 3 3.4 O=S(=O)(Nc1ccc([C@]23CNC[C@H]2C3)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1224700 16296 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 382 4 2 3 3.4 O=S(=O)(Nc1ccc([C@]23CNC[C@H]2C3)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.073
44454351 160701 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL411293 160701 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
44627120 6046 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
CHEMBL1080489 6046 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
49781039 17591 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
CHEMBL1258153 17591 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
44454167 95361 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 8 0 9 5.2 COCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256472 95361 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 8 0 9 5.2 COCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454192 97539 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL270239 97539 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454400 97653 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 7 4.9 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL270853 97653 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 7 4.9 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454309 97692 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 514 6 1 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271066 97692 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 514 6 1 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454219 155157 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 8 5.5 CCc1nc2cc3c(c(C)c2o1)CCN(CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL401777 155157 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 8 5.5 CCc1nc2cc3c(c(C)c2o1)CCN(CCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
46882054 6243 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1081491 6243 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)cc1 10.1016/j.bmcl.2010.01.090
45268999 198437 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 378 4 0 4 3.9 Cc1nc2cc(N3CCN(CCN4Cc5ccccc5C4)C3=O)ccc2s1 10.1016/j.bmcl.2009.06.028
CHEMBL559780 198437 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 378 4 0 4 3.9 Cc1nc2cc(N3CCN(CCN4Cc5ccccc5C4)C3=O)ccc2s1 10.1016/j.bmcl.2009.06.028
44454278 95594 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 454 6 1 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL257536 95594 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 454 6 1 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C 10.1016/j.bmcl.2007.12.066
11641641 97560 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 487 6 0 7 5.2 Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1 10.1016/j.bmcl.2007.12.042
CHEMBL270387 97560 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 487 6 0 7 5.2 Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1 10.1016/j.bmcl.2007.12.042
45270903 199190 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 347 4 0 2 3.7 O=C1N(CCN2C[C@H]3CC[C@H](CC3)C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL565075 199190 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 347 4 0 2 3.7 O=C1N(CCN2C[C@H]3CC[C@H](CC3)C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
44626527 5889 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
CHEMBL1079494 5889 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
44627024 5946 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2C[C@H]3C[C@@]3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079823 5946 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 451 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2C[C@H]3C[C@@]3(c3ccc(C(C)(C)C)cc3)C2)n1C 10.1021/jm901319p
44627242 6120 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1080846 6120 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.8 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)c(Cl)c3)C2)n1C 10.1021/jm901319p
49781040 17624 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 495 8 1 7 5.1 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4F)CC23)n1C 10.1021/jm100832d
CHEMBL1258268 17624 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 495 8 1 7 5.1 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4F)CC23)n1C 10.1021/jm100832d
11627847 95269 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256015 95269 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11613587 97703 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 542 7 0 9 5.2 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(F)(F)C(F)(F)F)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL271083 97703 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 542 7 0 9 5.2 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(C(F)(F)C(F)(F)F)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
45271520 197400 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 400 6 0 4 2.9 CC(C)N1CCN(CCN2CCN(c3cccc(OC(F)(F)F)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL549894 197400 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 400 6 0 4 2.9 CC(C)N1CCN(CCN2CCN(c3cccc(OC(F)(F)F)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
23631000 92907 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 527 7 0 7 6.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C(F)(F)F)cc4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243897 92907 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 527 7 0 7 6.0 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C(F)(F)F)cc4)n2C)CC3)no1 10.1021/jm0705612
23630797 93155 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 465 7 0 8 5.1 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccs4)n2C)CC3)o1 10.1021/jm0705612
CHEMBL244275 93155 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 465 7 0 8 5.1 Cc1cnc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4cccs4)n2C)CC3)o1 10.1021/jm0705612
23630604 144283 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1ccccc1-c1nnc(SCCCN2CCc3ccc(-c4cc(C)on4)cc3CC2)n1C 10.1021/jm0705612
CHEMBL390429 144283 None 0 Human Functional pKi = 8.5 8.5 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 489 8 0 8 5.0 COc1ccccc1-c1nnc(SCCCN2CCc3ccc(-c4cc(C)on4)cc3CC2)n1C 10.1021/jm0705612
46882458 5980 None 0 Human Functional pKi = 8.4 8.4 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1080046 5980 None 0 Human Functional pKi = 8.4 8.4 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
143 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
5311096 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
CHEMBL85606 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
49865623 16038 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc(C34CNCC3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223657 16038 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 356 5 2 3 3.5 CC(C)c1ccc(S(=O)(=O)Nc2ccc(C34CNCC3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
11497680 97905 None 7 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL272150 97905 None 7 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11721190 155364 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL402853 155364 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11677768 155664 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 502 6 0 8 4.9 Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL404404 155664 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 502 6 0 8 4.9 Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
143 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2009.06.043
5311096 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2009.06.043
CHEMBL85606 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2009.06.043
143 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm901319p
5311096 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm901319p
CHEMBL85606 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm901319p
44626639 5890 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 533 7 0 6 5.9 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Br)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1079497 5890 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 533 7 0 6 5.9 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Br)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627353 6364 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
CHEMBL1082111 6364 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cc(C(F)(F)F)ccc3F)C2)n1C 10.1021/jm901319p
11497680 97905 None 7 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL272150 97905 None 7 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1021/jm901319p
52947694 17493 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)CC2)n1C 10.1021/jm100832d
CHEMBL1257809 17493 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)CC2)n1C 10.1021/jm100832d
52949300 17529 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 521 7 0 7 6.1 Cc1nc(C)c(-c2nnc(SCCCN3CCC4CC4(c4ccc(C(F)(F)F)cc4)CC3)n2C)s1 10.1021/jm100832d
CHEMBL1257926 17529 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 521 7 0 7 6.1 Cc1nc(C)c(-c2nnc(SCCCN3CCC4CC4(c4ccc(C(F)(F)F)cc4)CC3)n2C)s1 10.1021/jm100832d
52940961 17557 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 488 7 0 7 4.8 Cn1c(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)CC2)nnc1-c1ccnnc1 10.1021/jm100832d
CHEMBL1258034 17557 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 488 7 0 7 4.8 Cn1c(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)CC2)nnc1-c1ccnnc1 10.1021/jm100832d
49780809 17558 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
CHEMBL1258035 17558 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 8 1 7 5.0 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC[C@]3(c4ccc(C(F)(F)F)cc4)CC23)n1C 10.1021/jm100832d
143 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
5311096 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
CHEMBL85606 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
11576387 95179 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 468 7 0 9 4.5 CCc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL255567 95179 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 468 7 0 9 4.5 CCc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
11526451 155151 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 518 7 0 11 4.2 Cc1cc(-c2nc3cc4c(cc3o2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)CC4)n(C)n1 10.1016/j.bmcl.2007.12.066
CHEMBL401728 155151 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 518 7 0 11 4.2 Cc1cc(-c2nc3cc4c(cc3o2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)CC4)n(C)n1 10.1016/j.bmcl.2007.12.066
11548217 155356 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 8 0 8 6.0 CCCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL402826 155356 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 8 0 8 6.0 CCCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
46882005 5848 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 307 3 0 2 3.1 CN1CCCCC1CN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2010.01.090
CHEMBL1079190 5848 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 307 3 0 2 3.1 CN1CCCCC1CN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2010.01.090
46881463 7220 None 0 Human Functional pKi = 8.4 8.4 - 3
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1085672 7220 None 0 Human Functional pKi = 8.4 8.4 - 3
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
45272434 200179 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 341 5 0 4 1.8 CC(C)N1CCN(CCN2CCN(c3cccc(C#N)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL571456 200179 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 341 5 0 4 1.8 CC(C)N1CCN(CCN2CCN(c3cccc(C#N)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
143 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm0705612
5311096 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm0705612
CHEMBL85606 3515 None 36 Human Functional pKi = 8.4 8.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1021/jm0705612
23631636 92906 None 0 Human Functional pKi = 8.4 8.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 484 7 0 8 4.9 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C#N)cc4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243896 92906 None 0 Human Functional pKi = 8.4 8.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 484 7 0 8 4.9 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C#N)cc4)n2C)CC3)no1 10.1021/jm0705612
46882521 5713 None 0 Human Functional pKi = 7.5 7.5 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5713 None 0 Human Functional pKi = 7.5 7.5 - 2
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
11577158 97860 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL271909 97860 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
45271760 198016 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 399 6 0 3 4.9 CN(CCN1CCN(c2cccc(Cl)c2)C1=O)Cc1cc2ccccc2s1 10.1016/j.bmcl.2009.06.043
CHEMBL554738 198016 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 399 6 0 3 4.9 CN(CCN1CCN(c2cccc(Cl)c2)C1=O)Cc1cc2ccccc2s1 10.1016/j.bmcl.2009.06.043
44626641 5903 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 480 7 0 7 5.0 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C#N)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1079577 5903 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 480 7 0 7 5.0 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(C#N)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44626738 5904 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079578 5904 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
44627238 6002 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccccc3C(F)(F)F)C2)n1C 10.1021/jm901319p
CHEMBL1080189 6002 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccccc3C(F)(F)F)C2)n1C 10.1021/jm901319p
24758832 17731 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1ccc2c(c1)C1(CCC2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
CHEMBL1258605 17731 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1ccc2c(c1)C1(CCC2)CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
24758947 17806 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 473 6 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5ccc(Cl)cc54)C3)n2C)s1 10.1021/jm100832d
CHEMBL1258834 17806 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 473 6 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5ccc(Cl)cc54)C3)n2C)s1 10.1021/jm100832d
24758481 17835 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 473 6 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5cc(Cl)ccc54)C3)n2C)s1 10.1021/jm100832d
CHEMBL1258948 17835 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 473 6 0 7 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5cc(Cl)ccc54)C3)n2C)s1 10.1021/jm100832d
52945023 55296 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 495 8 1 7 5.1 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm100832d
CHEMBL1258269 55296 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 495 8 1 7 5.1 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm100832d
CHEMBL1618255 55296 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 495 8 1 7 5.1 Cc1ncoc1-c1nnc(SCCCN[C@@H]2CC3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm100832d
11496746 95398 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 484 5 0 8 5.0 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256650 95398 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 484 5 0 8 5.0 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11511117 97488 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 469 6 0 7 4.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(F)c(F)c2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL269995 97488 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 469 6 0 7 4.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(F)c(F)c2)n1C)CC3 10.1016/j.bmcl.2007.12.066
11539722 97985 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 452 7 0 9 4.1 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272546 97985 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 452 7 0 9 4.1 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
11692214 155155 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 5.9 CCc1nc2cc3c(c(C)c2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL401752 155155 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 5.9 CCc1nc2cc3c(c(C)c2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454150 155531 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 532 6 0 8 6.0 Cc1ccc2c(-c3nnc(SCCCN4CCc5c(Cl)cc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL403815 155531 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 532 6 0 8 6.0 Cc1ccc2c(-c3nnc(SCCCN4CCc5c(Cl)cc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
24849462 202214 None 0 Human Functional pKi = 6.5 6.5 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593744 202214 None 0 Human Functional pKi = 6.5 6.5 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
44627468 6291 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081747 6291 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
44454218 95680 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 5 0 8 5.3 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257901 95680 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 5 0 8 5.3 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454402 97695 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 452 7 0 9 4.2 Cc1nc2cc3c(cc2o1)CCN(CCCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL271073 97695 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 452 7 0 9 4.2 Cc1nc2cc3c(cc2o1)CCN(CCCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
44454275 155209 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 562 5 0 8 5.7 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL402015 155209 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 562 5 0 8 5.7 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454247 157812 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 616 5 0 8 6.5 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL408208 157812 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 616 5 0 8 6.5 Cc1ccc2c(-c3nnc(SCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46881412 6859 None 0 Human Functional pKi = 6.5 6.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 357 4 0 3 2.6 O=S1(=O)N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1084121 6859 None 0 Human Functional pKi = 6.5 6.5 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 357 4 0 3 2.6 O=S1(=O)N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
45269235 198865 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 373 6 0 2 4.2 CN(CCN1CCN(c2ccc(F)cc2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
CHEMBL562836 198865 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 373 6 0 2 4.2 CN(CCN1CCN(c2ccc(F)cc2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
44626740 5992 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1080117 5992 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44626734 6194 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081237 6194 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 523 7 0 6 6.4 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)c(Cl)c5)C4)n3C)cccc2n1 10.1021/jm901319p
52941427 17457 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4ccc(C(F)(F)F)cc4)CC3C2)n1C 10.1021/jm100832d
CHEMBL1257686 17457 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4ccc(C(F)(F)F)cc4)CC3C2)n1C 10.1021/jm100832d
11547466 95186 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 478 8 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(CC5CC5)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL255619 95186 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 478 8 0 9 4.5 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4nc(CC5CC5)oc4cc3CC2)n1C 10.1016/j.bmcl.2007.12.066
11585248 95367 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 604 8 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256482 95367 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 604 8 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11627879 95400 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 6 0 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256652 95400 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 528 6 0 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11613873 95728 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 566 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(CC(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL258090 95728 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 566 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(CC(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11606456 97652 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 8 0 7 5.7 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL270852 97652 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 8 0 7 5.7 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6c(cc5CC4)C(=O)N(C(C)C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11664328 97694 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 590 7 0 8 6.5 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271072 97694 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 590 7 0 8 6.5 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11663504 98023 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 8 5.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272694 98023 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 8 5.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454401 155230 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 6 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL402087 155230 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 554 6 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
45270702 197681 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 393 4 0 2 4.0 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(Cl)c1F 10.1016/j.bmcl.2009.06.028
CHEMBL550849 197681 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 393 4 0 2 4.0 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(Cl)c1F 10.1016/j.bmcl.2009.06.028
45268990 198384 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 365 6 0 3 3.7 CC(C)Oc1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL559386 198384 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 365 6 0 3 3.7 CC(C)Oc1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
23630503 92909 None 0 Human Functional pKi = 7.4 7.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 397 6 0 7 3.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243899 92909 None 0 Human Functional pKi = 7.4 7.4 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 397 6 0 7 3.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C)n2C)CC3)no1 10.1021/jm0705612
44454318 97779 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 491 6 0 9 4.0 Cc1ncoc1-c1nnc(SCCCN2CCc3nc4ccc(C(F)(F)F)cn4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL271511 97779 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 491 6 0 9 4.0 Cc1ncoc1-c1nnc(SCCCN2CCc3nc4ccc(C(F)(F)F)cn4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
44627131 5978 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1079980 5978 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(F)c3)C2)n1C 10.1021/jm901319p
44627025 6362 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1082106 6362 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 473 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Br)cc3)C2)n1C 10.1021/jm901319p
46225583 202630 None 0 Human Functional pKi = 5.4 5.4 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596527 202630 None 0 Human Functional pKi = 5.4 5.4 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
121304574 143120 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3894853 143120 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
16123353 16025 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 370 7 2 3 3.7 CCCCc1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223601 16025 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 370 7 2 3 3.7 CCCCc1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
11642163 97558 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 522 6 0 9 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1 10.1016/j.bmcl.2007.12.042
CHEMBL270376 97558 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 522 6 0 9 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1 10.1016/j.bmcl.2007.12.042
11497679 155654 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL404363 155654 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
45273545 198956 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 385 7 0 3 4.1 COc1cccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)c1 10.1016/j.bmcl.2009.06.043
CHEMBL563435 198956 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 385 7 0 3 4.1 COc1cccc(N2CCN(CCN(C)C[C@]34CC[C@H](CC3)C4(C)C)C2=O)c1 10.1016/j.bmcl.2009.06.043
44627127 5881 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
CHEMBL1079461 5881 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(Cl)c3)C2)n1C 10.1021/jm901319p
44626527 5889 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
CHEMBL1079494 5889 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 459 8 0 8 4.2 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1Cl 10.1021/jm901319p
44627033 5950 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079837 5950 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)cc1 10.1021/jm901319p
44627131 5978 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1079980 5978 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(F)c3)C2)n1C 10.1021/jm901319p
44626632 6188 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 455 7 0 6 5.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccccc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1081203 6188 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 455 7 0 6 5.1 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccccc5)C4)n3C)cccc2n1 10.1021/jm901319p
49781255 17766 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4cc(Br)ccc43)C2)n1C 10.1021/jm100832d
CHEMBL1258712 17766 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4cc(Br)ccc43)C2)n1C 10.1021/jm100832d
11555971 95224 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 567 7 0 9 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(N7CCCCC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255826 95224 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 567 7 0 9 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(N7CCCCC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11628631 97536 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(F)(F)C(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL270227 97536 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(F)(F)C(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882004 5606 None 0 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1077344 5606 None 0 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
45268141 198450 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 425 5 0 3 4.1 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
CHEMBL559919 198450 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 425 5 0 3 4.1 O=C1N(CCN2CCC(C(F)(F)F)CC2)CCN1c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.06.028
11705570 92261 None 0 Human Functional pKi = 8.3 8.3 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 474 6 0 9 3.5 Cc1cnc(-c2nnc(SCCN3CCc4ccc(-c5cc(C)nn5C)cc4CC3)n2C)cn1 10.1021/jm0705612
CHEMBL242601 92261 None 0 Human Functional pKi = 8.3 8.3 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 474 6 0 9 3.5 Cc1cnc(-c2nnc(SCCN3CCc4ccc(-c5cc(C)nn5C)cc4CC3)n2C)cn1 10.1021/jm0705612
23631093 92625 None 0 Human Functional pKi = 8.3 8.3 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 439 6 0 7 4.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(C)(C)C)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243474 92625 None 0 Human Functional pKi = 8.3 8.3 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 439 6 0 7 4.7 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(C(C)(C)C)n2C)CC3)no1 10.1021/jm0705612
45268345 198592 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 417 5 0 2 5.1 O=C1N(CCN2CCC(c3ccc(Cl)cc3)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL561128 198592 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 417 5 0 2 5.1 O=C1N(CCN2CCC(c3ccc(Cl)cc3)CC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
45268373 199100 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 399 6 0 4 3.8 CN(CCN1CCN(c2ccc3c(c2)OCO3)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
CHEMBL564347 199100 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 399 6 0 4 3.8 CN(CCN1CCN(c2ccc3c(c2)OCO3)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
44626935 6256 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2C[C@H]3C[C@@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081580 6256 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 463 7 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2C[C@H]3C[C@@]3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
44626530 6329 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081934 6329 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(OC(F)(F)F)c3)C2)n1C 10.1021/jm901319p
44627240 6332 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1081966 6332 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 479 8 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(OC(F)(F)F)cc3)C2)n1C 10.1021/jm901319p
24758945 17309 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 457 6 0 7 4.8 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5ccc(F)cc54)C3)n2C)s1 10.1021/jm100832d
CHEMBL1257214 17309 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 457 6 0 7 4.8 Cc1nc(C)c(-c2nnc(SCCCN3CCC4(CCc5ccc(F)cc54)C3)n2C)s1 10.1021/jm100832d
49780808 17341 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 8 1 7 4.0 Cc1ncoc1-c1nnc(SCCCNC2CC3CC3(c3ccccc3)C2)n1C 10.1021/jm100832d
CHEMBL1257335 17341 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 409 8 1 7 4.0 Cc1ncoc1-c1nnc(SCCCNC2CC3CC3(c3ccccc3)C2)n1C 10.1021/jm100832d
49781477 17343 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.7 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2cccc(C(F)(F)F)c2)C3)n1C 10.1021/jm100832d
CHEMBL1257337 17343 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 491 7 0 7 5.7 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2cccc(C(F)(F)F)c2)C3)n1C 10.1021/jm100832d
11641596 97851 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 484 6 0 8 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271844 97851 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 484 6 0 8 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11526531 98024 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C7CC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272695 98024 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 524 7 0 8 5.9 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C7CC7)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11527195 98111 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 590 6 0 8 6.5 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL273165 98111 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 590 6 0 8 6.5 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11606435 155210 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL402016 155210 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(F)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882050 6239 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 317 5 0 3 2.8 COc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081487 6239 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 317 5 0 3 2.8 COc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
46225569 203819 None 0 Human Functional pKi = 6.3 6.3 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL604467 203819 None 0 Human Functional pKi = 6.3 6.3 - 2
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
44627129 5882 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079462 5882 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
44627123 6047 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1080490 6047 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 429 7 0 7 4.2 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3)C2)n1C 10.1021/jm901319p
45272411 197338 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 388 4 0 4 3.6 CC(=O)n1ccc2cc(N3CCN(CCN4Cc5ccccc5C4)C3=O)ccc21 10.1016/j.bmcl.2009.06.028
CHEMBL549759 197338 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 388 4 0 4 3.6 CC(=O)n1ccc2cc(N3CCN(CCN4Cc5ccccc5C4)C3=O)ccc21 10.1016/j.bmcl.2009.06.028
45269860 197749 None 1 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccccc1Cl 10.1016/j.bmcl.2009.06.028
CHEMBL551386 197749 None 1 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 355 5 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccccc1Cl 10.1016/j.bmcl.2009.06.028
45272425 199148 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 403 5 0 2 4.5 CC(c1cccc(C(F)(F)F)c1)N1CCN(CCN2Cc3ccccc3C2)C1=O 10.1016/j.bmcl.2009.06.028
CHEMBL564741 199148 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 403 5 0 2 4.5 CC(c1cccc(C(F)(F)F)c1)N1CCN(CCN2Cc3ccccc3C2)C1=O 10.1016/j.bmcl.2009.06.028
46190877 1871 None 8 Human Functional pKi = 5.3 5.3 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
6252 1871 None 8 Human Functional pKi = 5.3 5.3 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
CHEMBL605836 1871 None 8 Human Functional pKi = 5.3 5.3 - 1
Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
121315259 148389 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 463 6 0 7 4.8 Cc1ncoc1-c1nnc(SCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3936812 148389 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 463 6 0 7 4.8 Cc1ncoc1-c1nnc(SCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
16123462 16026 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 384 6 2 3 4.0 CCC(C)(C)c1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223602 16026 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 384 6 2 3 4.0 CCC(C)(C)c1ccc(S(=O)(=O)Nc2ccc([C@]34CNC[C@H]3C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
16123241 16284 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 370 5 1 3 3.8 CC(C)c1ccc(S(=O)(=O)Nc2ccc([C@@]34C[C@@H]3CN(C)C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1224639 16284 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 370 5 1 3 3.8 CC(C)c1ccc(S(=O)(=O)Nc2ccc([C@@]34C[C@@H]3CN(C)C4)cc2)cc1 10.1016/j.bmcl.2010.07.073
11533473 97604 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 503 6 0 9 4.3 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL270602 97604 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 503 6 0 9 4.3 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
44454418 155527 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 468 7 0 9 4.5 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL403804 155527 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 468 7 0 9 4.5 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.042
45272634 198930 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 6 0 2 4.7 CN(CCN1CCN(c2cccc(Cl)c2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
CHEMBL563274 198930 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 6 0 2 4.7 CN(CCN1CCN(c2cccc(Cl)c2)C1=O)C[C@]12CC[C@H](CC1)C2(C)C 10.1016/j.bmcl.2009.06.043
44627129 5882 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079462 5882 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
44626738 5904 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
CHEMBL1079578 5904 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 485 8 0 7 5.1 COc1ccc(C23CC2CN(CCCSc2nnc(-c4cccc5nc(C)ccc45)n2C)C3)cc1 10.1021/jm901319p
44626740 5992 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL1080117 5992 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 489 7 0 6 5.7 Cc1ccc2c(-c3nnc(SCCCN4CC5CC5(c5ccc(Cl)cc5)C4)n3C)cccc2n1 10.1021/jm901319p
44627468 6291 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
CHEMBL1081747 6291 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 447 7 0 7 4.3 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(Cl)cc3F)C2)n1C 10.1021/jm901319p
49781478 17378 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 509 7 0 7 5.8 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(F)(F)F)cc2F)C3)n1C 10.1021/jm100832d
CHEMBL1257448 17378 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 509 7 0 7 5.8 Cc1ncoc1-c1nnc(SCCCN2[C@H]3CC[C@@H]2C[C@H](c2ccc(C(F)(F)F)cc2F)C3)n1C 10.1021/jm100832d
52940753 17492 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4cccc(C(F)(F)F)c4)CC3C2)n1C 10.1021/jm100832d
CHEMBL1257808 17492 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3(c4cccc(C(F)(F)F)c4)CC3C2)n1C 10.1021/jm100832d
11656848 95362 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256473 95362 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(F)F)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11699340 95366 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256481 95366 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 526 7 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
45273334 195379 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 349 5 0 2 4.1 CC(C)c1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
CHEMBL540241 195379 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 349 5 0 2 4.1 CC(C)c1cccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)c1 10.1016/j.bmcl.2009.06.028
45272426 197898 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.3 CC1CCCN(CCN2CCN(c3cccc(Cl)c3)C2=O)C1 10.1016/j.bmcl.2009.06.028
CHEMBL552371 197898 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.3 CC1CCCN(CCN2CCN(c3cccc(Cl)c3)C2=O)C1 10.1016/j.bmcl.2009.06.028
45268119 199185 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(Cl)ccc1F 10.1016/j.bmcl.2009.06.028
CHEMBL565031 199185 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 359 4 0 2 3.7 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cc(Cl)ccc1F 10.1016/j.bmcl.2009.06.028
23630998 92870 None 0 Human Functional pKi = 8.2 8.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 539 7 0 9 5.6 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc5nc(C)c(C)nc5c4)n2C)CC3)no1 10.1021/jm0705612
CHEMBL243708 92870 None 0 Human Functional pKi = 8.2 8.2 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 539 7 0 9 5.6 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc5nc(C)c(C)nc5c4)n2C)CC3)no1 10.1021/jm0705612
121304424 143931 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3901587 143931 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
121304458 154078 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3983937 154078 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor expressed in CHO cell membranes after 90 mins in presence of quinelorane by [35S]-GTPgammaS binding assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
11656243 97970 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL272511 97970 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11518933 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
CHEMBL269959 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
11656243 97970 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
CHEMBL272511 97970 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2009.06.043
44627355 5968 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
CHEMBL1079938 5968 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3cccc(C(F)(F)F)c3F)C2)n1C 10.1021/jm901319p
11518933 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1021/jm901319p
CHEMBL269959 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1021/jm901319p
11669953 95593 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 468 6 0 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL257534 95593 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 468 6 0 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C 10.1016/j.bmcl.2007.12.066
11518933 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL269959 97477 None 7 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11548755 97708 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 580 7 0 8 6.8 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271097 97708 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 580 7 0 8 6.8 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882052 6241 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
CHEMBL1081489 6241 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
45273272 198117 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 3 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc2sccc2c1 10.1016/j.bmcl.2009.06.028
CHEMBL556478 198117 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 363 4 0 3 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1c1ccc2sccc2c1 10.1016/j.bmcl.2009.06.028
45268127 199115 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 322 4 0 3 2.6 Cc1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)cn1 10.1016/j.bmcl.2009.06.028
CHEMBL564477 199115 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 322 4 0 3 2.6 Cc1ccc(N2CCN(CCN3Cc4ccccc4C3)C2=O)cn1 10.1016/j.bmcl.2009.06.028
46882583 5758 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
CHEMBL1078491 5758 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
45102708 5772 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078595 5772 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at dopamine D3 receptorAgonist activity at dopamine D3 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
16123464 16297 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 398 5 2 4 3.2 O=S(=O)(Nc1ccc([C@]23CNC[C@H]2C3)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.07.073
CHEMBL1224701 16297 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 398 5 2 4 3.2 O=S(=O)(Nc1ccc([C@]23CNC[C@H]2C3)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.07.073
45273523 198122 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 413 6 0 3 4.5 COc1cccc(C2CCCN(CCN3CCN(c4cccc(Cl)c4)C3=O)C2)c1 10.1016/j.bmcl.2009.06.043
CHEMBL556496 198122 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 413 6 0 3 4.5 COc1cccc(C2CCCN(CCN3CCN(c4cccc(Cl)c4)C3=O)C2)c1 10.1016/j.bmcl.2009.06.043
44454434 97960 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 7 4.5 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272480 97960 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 512 6 0 7 4.5 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
45272412 198022 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 5 0 2 2.9 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccccc1 10.1016/j.bmcl.2009.06.028
CHEMBL554914 198022 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 5 0 2 2.9 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccccc1 10.1016/j.bmcl.2009.06.028
16123140 16293 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 384 6 1 3 4.2 CCN1C[C@H]2C[C@@]2(c2ccc(NS(=O)(=O)c3ccc(C(C)C)cc3)cc2)C1 10.1016/j.bmcl.2010.07.073
CHEMBL1224697 16293 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 384 6 1 3 4.2 CCN1C[C@H]2C[C@@]2(c2ccc(NS(=O)(=O)c3ccc(C(C)C)cc3)cc2)C1 10.1016/j.bmcl.2010.07.073
11519133 169526 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL442456 169526 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 512 7 0 8 5.6 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
44627129 5882 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
CHEMBL1079462 5882 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 413 7 0 7 3.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)cc3)C2)n1C 10.1021/jm901319p
44627120 6046 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
CHEMBL1080489 6046 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 425 8 0 8 3.5 COc1cccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c1 10.1021/jm901319p
49836026 17418 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm100832d
CHEMBL1257566 17418 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 477 7 0 7 4.9 Cc1ncoc1-c1nnc(SCCCN2CCC3CC3(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/jm100832d
24758828 17657 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 501 6 0 7 5.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCCc4cc(Br)ccc43)C2)n1C 10.1021/jm100832d
CHEMBL1258380 17657 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 501 6 0 7 5.0 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCCc4cc(Br)ccc43)C2)n1C 10.1021/jm100832d
24758717 17767 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4c(Br)cccc43)C2)n1C 10.1021/jm100832d
CHEMBL1258713 17767 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 487 6 0 7 4.6 Cc1ncoc1-c1nnc(SCCCN2CCC3(CCc4c(Br)cccc43)C2)n1C 10.1021/jm100832d
11628452 97594 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(-c7cc(C)nn7C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL270567 97594 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(-c7cc(C)nn7C)oc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11591633 97707 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 515 7 0 7 5.8 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL271096 97707 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 515 7 0 7 5.8 CCc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
11584185 157772 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 500 6 1 8 4.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCCN6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL408169 157772 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 500 6 1 8 4.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCCN6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
45271516 197984 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 384 4 0 3 3.2 N#Cc1cc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)ccc1F 10.1016/j.bmcl.2009.06.028
CHEMBL554073 197984 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 384 4 0 3 3.2 N#Cc1cc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)ccc1F 10.1016/j.bmcl.2009.06.028
45268148 198540 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 350 5 0 3 2.6 CC(C)N1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
CHEMBL560715 198540 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 350 5 0 3 2.6 CC(C)N1CCN(CCN2CCN(c3cccc(Cl)c3)C2=O)CC1 10.1016/j.bmcl.2009.06.028
45267270 198581 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.5 CC1CCCCN1CCN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.028
CHEMBL561054 198581 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 321 4 0 2 3.5 CC1CCCCN1CCN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.028
11584694 144533 None 0 Human Functional pKi = 8.1 8.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 540 7 0 7 5.8 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C(F)(F)F)cc4)n2C)CC3)n(C)n1 10.1021/jm0705612
CHEMBL390649 144533 None 0 Human Functional pKi = 8.1 8.1 - 0
Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 minsDisplacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins
ChEMBL 540 7 0 7 5.8 Cc1cc(-c2ccc3c(c2)CCN(CCCSc2nnc(-c4ccc(C(F)(F)F)cc4)n2C)CC3)n(C)n1 10.1021/jm0705612
49865589 16023 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 328 4 1 3 2.4 CN(c1ccc([C@]23CNC[C@H]2C3)cc1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.07.073
CHEMBL1223599 16023 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 328 4 1 3 2.4 CN(c1ccc([C@]23CNC[C@H]2C3)cc1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.07.073
45273510 198056 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 309 4 0 3 2.6 COC[C@@H]1CCCN1N1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.043
CHEMBL555744 198056 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 309 4 0 3 2.6 COC[C@@H]1CCCN1N1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2009.06.043
44627351 6257 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
CHEMBL1081587 6257 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2CC3CC3(c3ccc(F)c(C(F)(F)F)c3)C2)n1C 10.1021/jm901319p
44627466 6318 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 427 7 0 7 4.0 Cc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c(F)c1 10.1021/jm901319p
CHEMBL1081869 6318 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assayAntagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay
ChEMBL 427 7 0 7 4.0 Cc1ccc(C23CC2CN(CCCSc2nnc(-c4ocnc4C)n2C)C3)c(F)c1 10.1021/jm901319p
24758836 17696 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1cccc2c1CCCC21CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
CHEMBL1258493 17696 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS bindingAntagonist activity at human dopamine D3 expressed in CHO cells assessed as inhibition of quinelorane-induced [35S]GTPgammaS binding
ChEMBL 453 7 0 8 4.2 COc1cccc2c1CCCC21CCN(CCCSc2nnc(-c3ocnc3C)n2C)C1 10.1021/jm100832d
11568714 95360 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 454 6 0 9 4.3 Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256471 95360 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 454 6 0 9 4.3 Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
11497924 95591 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 580 6 0 8 6.8 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257525 95591 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assayAntagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay
ChEMBL 580 6 0 8 6.8 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
46882006 5849 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1079191 5849 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.090
46882009 6216 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081311 6216 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
46881409 6761 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 288 4 0 3 2.2 O=C1N(CCN2CCCCCC2)CCN1c1cccnc1 10.1016/j.bmcl.2010.01.090
CHEMBL1083814 6761 None 0 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assayAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinperol-induced [35S]GTPgamma binding by scintillation proximity affinity assay
ChEMBL 288 4 0 3 2.2 O=C1N(CCN2CCCCCC2)CCN1c1cccnc1 10.1016/j.bmcl.2010.01.090
45267261 198534 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.06.028
CHEMBL560650 198534 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometryAntagonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTP-gamma-S-based scintillation spectrometry
ChEMBL 389 5 0 2 4.2 O=C1N(CCN2Cc3ccccc3C2)CCN1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.06.028
44454443 97816 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 449 6 0 9 3.6 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL271702 97816 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assayAntagonist activity at dopamine D3 receptor by GTPgammaS binding assay
ChEMBL 449 6 0 9 3.6 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
16078 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
16078.0 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
2424 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
4109 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
CHEMBL465 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
DB00470 1362 None 15 Human Functional pEC50 = 8.1 8.1 -1 7
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Drug Central 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C None
119570 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570.0 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 None 58 Human Functional pEC50 = 8.1 8.1 -2 11
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2105 3054 None 28 Human Functional pEC50 = 8.1 8.1 -1 25
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 None 28 Human Functional pEC50 = 8.1 8.1 -1 25
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 None 28 Human Functional pEC50 = 8.1 8.1 -1 25
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 None 28 Human Functional pEC50 = 8.1 8.1 -1 25
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 None 28 Human Functional pEC50 = 8.1 8.1 -1 25
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
30699 220190 None 0 Human Functional pIC50 = 8.3 8.3 -1 14
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
4223 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314.0 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 None 57 Rat Functional pIC50 = 8.2 8.2 -97 17
Inhibition of rat dopamine D3 receptorInhibition of rat dopamine D3 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
4223 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314.0 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 None 57 Human Functional pIC50 = 8.2 8.2 -97 17
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
100 3805 None 44 Human Functional pIC50 = 8.1 8.1 -4 38
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 None 44 Human Functional pIC50 = 8.1 8.1 -4 38
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 None 44 Human Functional pIC50 = 8.1 8.1 -4 38
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 None 44 Human Functional pIC50 = 8.1 8.1 -4 38
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 None 44 Human Functional pIC50 = 8.1 8.1 -4 38
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 None 70 Rat Functional pIC50 = 8.1 8.1 -4 33
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
11154555 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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
11154555.0 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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
CHEMBL3085826 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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 800 None 50 Rat Functional pIC50 = 8.1 8.1 -1 10
NoneNone
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
10263487 3069 None 0 Human Functional pIC50 = 6.7 6.7 19 2
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105
7683 3069 None 0 Human Functional pIC50 = 6.7 6.7 19 2
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105
4223 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
6918314 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
6918314.0 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
7427 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
CHEMBL439849 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
DB06684 3992 None 57 Human Functional pIC50 = 7.2 7.2 -97 17
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

681 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
681.0 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
940 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
947 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL59 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00988 1465 None 47 Human Binding pAC50 = 9.4 9.4 -8 38
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
2407 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227.0 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3372 None 50 Human Binding pAC50 = 8.0 8.0 -5 7
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
1222 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396.0 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1664 None 37 Human Binding pAC50 = 7 7.0 -4 32
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
100 3805 None 44 Human Binding pAC50 = 7 7.0 -1 55
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 44 Human Binding pAC50 = 7 7.0 -1 55
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 44 Human Binding pAC50 = 7 7.0 -1 55
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 44 Human Binding pAC50 = 7 7.0 -1 55
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 44 Human Binding pAC50 = 7 7.0 -1 55
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
1802 2533 None 17 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 10.1038/s41467-023-40064-9
3342 2533 None 17 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 10.1038/s41467-023-40064-9
4192 2533 None 17 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 10.1038/s41467-023-40064-9
CHEMBL655 2533 None 17 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 10.1038/s41467-023-40064-9
DB00683 2533 None 17 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 10.1038/s41467-023-40064-9
4499 59795 None 61 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL1726 59795 None 61 Human Binding pAC50 = 5 5.0 - 2
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
4417 55578 None 40 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1439099 55578 None 40 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1620794 55578 None 40 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
25151352 140693 None 56 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 140693 None 56 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
57383420 109986 None 0 Human Binding pAC50 = 5.0 5.0 - 0
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234540 109986 None 0 Human Binding pAC50 = 5.0 5.0 - 0
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
2406 100458 None 56 Human Binding pAC50 = 5.0 5.0 -16 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
CHEMBL290106 100458 None 56 Human Binding pAC50 = 5.0 5.0 -16 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
2805 161984 None 27 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL415087 161984 None 27 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
31101 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
31101.0 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
35 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
403 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
CHEMBL493 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
DB01200 729 None 28 Human Binding pAC50 = 7.0 7.0 -9 35
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 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 10.1038/s41467-023-40064-9
3952 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646.0 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5443 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063.0 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL1331786 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL420 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
DB00629 1888 None 32 Human Binding pAC50 = 5.0 5.0 - 12
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
24821094 67115 None 58 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
CHEMBL1873475 67115 None 58 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
4021 100534 None 72 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 174 1 0 2 1.8 CC1=NN(c2ccccc2)C(=O)C1 10.1038/s41467-023-40064-9
CHEMBL290916 100534 None 72 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 174 1 0 2 1.8 CC1=NN(c2ccccc2)C(=O)C1 10.1038/s41467-023-40064-9
135398735 137055 None 20 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 137055 None 20 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 137055 None 20 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
2107 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747.0 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
9216 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL251940 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB01608 3055 None 44 Human Binding pAC50 = 8.0 8.0 - 1
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
133 2496 None 39 Human Binding pAC50 = 8.0 8.0 -8 42
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
1723 2496 None 39 Human Binding pAC50 = 8.0 8.0 -8 42
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
28693 2496 None 39 Human Binding pAC50 = 8.0 8.0 -8 42
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
CHEMBL19215 2496 None 39 Human Binding pAC50 = 8.0 8.0 -8 42
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
DB13520 2496 None 39 Human Binding pAC50 = 8.0 8.0 -8 42
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Binding pAC50 = 7.9 7.9 -26 67
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Binding pAC50 = 7.9 7.9 -3 85
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2435 3590 None 59 Human Binding pAC50 = 7.0 7.0 -8 48
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 59 Human Binding pAC50 = 7.0 7.0 -8 48
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 59 Human Binding pAC50 = 7.0 7.0 -8 48
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 59 Human Binding pAC50 = 7.0 7.0 -8 48
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 59 Human Binding pAC50 = 7.0 7.0 -8 48
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
1577 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
2537 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5355 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5501 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
643497 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
688272 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
688272.0 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
958 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
960 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL196677 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL26 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL267044 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB00391 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB16021 3703 None 66 Human Binding pAC50 = 7.0 7.0 -1 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Binding pAC50 = 7.0 7.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Binding pAC50 = 7.0 7.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Binding pAC50 = 7.0 7.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Binding pAC50 = 7.0 7.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2895 206050 None 27 Human Binding pAC50 = 6.0 6.0 - 8
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2895.0 206050 None 27 Human Binding pAC50 = 6.0 6.0 - 8
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 206050 None 27 Human Binding pAC50 = 6.0 6.0 - 8
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
DB00924 206050 None 27 Human Binding pAC50 = 6.0 6.0 - 8
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Binding pAC50 = 6.0 6.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Binding pAC50 = 6.0 6.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Binding pAC50 = 6.0 6.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Binding pAC50 = 6.0 6.0 -3235 20
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3561 19084 None 29 Human Binding pAC50 = 5.9 5.9 -1 11
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL1289 19084 None 29 Human Binding pAC50 = 5.9 5.9 -1 11
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
22530 56146 None 40 Human Binding pAC50 = 5.9 5.9 - 3
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1600878 56146 None 40 Human Binding pAC50 = 5.9 5.9 - 3
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1625607 56146 None 40 Human Binding pAC50 = 5.9 5.9 - 3
Binding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human DRD3 in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9