Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL3234540 drd3_human Human No 5.0 AC50 = 10200 nM Bind
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
424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21
CHEMBL3234544 drd3_human Human No 4.9 AC50 = 12900 nM Bind
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
410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1
CHEMBL3234542 drd3_human Human No 4.8 AC50 = 14500 nM Bind
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
391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21
CHEMBL3234537 drd3_human Human No 5.8 AC50 = 1620 nM Bind
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
429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21
CHEMBL3234522 drd3_human Human No 4.7 AC50 = 20400 nM Bind
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
410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21
CHEMBL3234527 drd3_human Human No 5.5 AC50 = 2890 nM Bind
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
434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21
CHEMBL3234536 drd3_human Human No 5.5 AC50 = 3240 nM Bind
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
422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21
CHEMBL3234539 drd3_human Human No 4.5 AC50 = 32400 nM Bind
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
468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21
CHEMBL3234541 drd3_human Human No 5.3 AC50 = 4570 nM Bind
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
468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21
CHEMBL3234543 drd3_human Human No 5.3 AC50 = 4570 nM Bind
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
397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21
CHEMBL1503220 drd3_human Human Yes 5.2 AC50 = 5760 nM Bind
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
434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21
CHEMBL3234538 drd3_human Human No 5.0 AC50 = 9130 nM Bind
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
496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21
CHEMBL346692 drd3_human Human No 10.6 EC50 = 0.0 nM Funct
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
444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL4285942 drd3_human Human No 10.6 EC50 = 0.0 nM Funct
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
444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL1765633 drd3_human Human No 10.3 EC50 = 0.1 nM Funct
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
430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1
CHEMBL468017 drd3_human Human No 10.2 EC50 = 0.1 nM Funct
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
467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1
CHEMBL399164 drd3_human Human No 10.1 EC50 = 0.1 nM Funct
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
423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1
CHEMBL467540 drd3_human Human No 10.1 EC50 = 0.1 nM Funct
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
475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1
CHEMBL514885 drd3_human Human No 10.1 EC50 = 0.1 nM Funct
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
475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL240773 drd3_human Human Yes 10.0 EC50 = 0.1 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL3125990 drd3_human Human No 10.0 EC50 = 0.1 nM Funct
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
491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL59 drd3_human Human Yes 10.0 EC50 = 0.1 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL250552 drd3_human Human No 9.9 EC50 = 0.1 nM Funct
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
393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1
CHEMBL273273 drd3_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC
CHEMBL4476784 drd3_human Human Yes 9.7 EC50 = 0.2 nM Bind
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL301265 drd3_rat Rat Yes 9.7 EC50 = 0.2 nM Funct
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
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL379602 drd3_human Human Yes 9.7 EC50 = 0.2 nM Funct
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
348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1
CHEMBL1254947 drd3_human Human No 9.6 EC50 = 0.3 nM Funct
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
469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2c(O)cccc2C1
CHEMBL2152747 drd3_human Human No 9.6 EC50 = 0.3 nM Funct
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
466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL2152746 drd3_human Human No 9.6 EC50 = 0.3 nM Funct
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
466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1
CHEMBL4071240 drd3_human Human No 9.5 EC50 = 0.3 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL4069145 drd3_human Human No 9.5 EC50 = 0.3 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=C(C=N4)/C=N/O)C=C3
CHEMBL4069145 drd3_human Human No 9.5 EC50 = 0.3 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=C(C=N4)/C=N/O)C=C3
CHEMBL4538230 drd3_human Human No 9.5 EC50 = 0.3 nM Funct
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
383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1
CHEMBL477206 drd3_human Human No 9.5 EC50 = 0.3 nM Funct
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
407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1
CHEMBL1256778 drd3_rat Rat Yes 9.4 EC50 = 0.4 nM Funct
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
249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21
CHEMBL70565 drd3_rat Rat Yes 9.4 EC50 = 0.4 nM Funct
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
249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21
CHEMBL424294 drd3_human Human Yes 9.4 EC50 = 0.4 nM Funct
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
423 8 1 5 4.2 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4S3
CHEMBL240773 drd3_human Human Yes 9.4 EC50 = 0.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL4078348 drd3_human Human No 9.4 EC50 = 0.4 nM Funct
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
393 9 1 5 4.5 CCCN(CCCCOC1=CC2=CC=NN2C=C1)[C@H]3CCC4=C(C3)C=CC=C4O
CHEMBL4078348 drd3_human Human No 9.4 EC50 = 0.4 nM Funct
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
393 9 1 5 4.5 CCCN(CCCCOC1=CC2=CC=NN2C=C1)[C@H]3CCC4=C(C3)C=CC=C4O
CHEMBL4097330 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
393 9 1 5 4.5 CCCN(CCCCOC1=CN2C(=CC=N2)C=C1)[C@H]3CCC4=C(C3)C=CC=C4O
CHEMBL4097330 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
393 9 1 5 4.5 CCCN(CCCCOC1=CN2C(=CC=N2)C=C1)[C@H]3CCC4=C(C3)C=CC=C4O
CHEMBL577073 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
450 7 1 7 3.7 CCCN(CCN1CCN(c2ccnc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL571992 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL569107 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
450 7 1 7 3.7 CCCN(CCN1CCN(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL2206264 drd3_human Human No 9.3 EC50 = 0.5 nM Funct
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
534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1
CHEMBL285755 drd3_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC
CHEMBL2152755 drd3_human Human No 9.3 EC50 = 0.6 nM Funct
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
466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL269004 drd3_human Human Yes 9.2 EC50 = 0.6 nM Funct
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
247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1
CHEMBL156639 drd3_human Human Yes 9.2 EC50 = 0.7 nM Funct
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
393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1
CHEMBL4073068 drd3_human Human No 9.1 EC50 = 0.7 nM Funct
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
386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21
CHEMBL599635 drd3_human Human No 9.1 EC50 = 0.7 nM Funct
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
460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1
CHEMBL4452046 drd3_human Human No 9.1 EC50 = 0.8 nM Funct
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
403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1
CHEMBL434665 drd3_human Human Yes 9.1 EC50 = 0.8 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
231 3 2 3 1.3 CCCN[C@@H]1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL571992 drd3_human Human No 9.1 EC50 = 0.8 nM Funct
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
450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL571992 drd3_human Human No 9.1 EC50 = 0.8 nM Funct
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
450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3742140 drd3_human Human No 9.1 EC50 = 0.8 nM Funct
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
469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3742430 drd3_human Human No 9.1 EC50 = 0.8 nM Funct
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
469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL2152752 drd3_human Human No 9.1 EC50 = 0.9 nM Funct
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
466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2c[nH]c3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL4071240 drd3_human Human No 9.1 EC50 = 0.9 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL4091498 drd3_human Human No 9.1 EC50 = 0.9 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4099236 drd3_human Human No 9.1 EC50 = 0.9 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4116199 drd3_human Human No 9.1 EC50 = 0.9 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4070196 drd3_human Human No 9.0 EC50 = 0.9 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL2206265 drd3_human Human No 9.0 EC50 = 0.9 nM Funct
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
548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1
CHEMBL285755 drd3_human Human Yes 9.0 EC50 = 1.0 nM Funct
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
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC
CHEMBL3597649 drd3_human Human No 9.0 EC50 = 1.0 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1
CHEMBL244990 drd3_human Human No 9.0 EC50 = 1 nM Funct
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
498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL301265 drd3_human Human Yes 9.0 EC50 = 1 nM Funct
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
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL155731 drd3_human Human Yes 9.0 EC50 = 1 nM Funct
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
246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N
CHEMBL4070196 drd3_human Human No 9.0 EC50 = 1 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL4092052 drd3_human Human No 9.0 EC50 = 1 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4092052 drd3_human Human No 9.0 EC50 = 1 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL1253770 drd3_human Human No 9.0 EC50 = 1.0 nM Funct
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
469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1
CHEMBL59 drd3_human Human Yes 9.0 EC50 = 1.1 nM Bind
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL339960 drd3_human Human No 9.0 EC50 = 1.1 nM Funct
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
444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL4287055 drd3_human Human No 9.0 EC50 = 1.1 nM Funct
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
444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL316983 drd3_human Human No 9.0 EC50 = 1.1 nM Bind
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1
CHEMBL316983 drd3_human Human No 9.0 EC50 = 1.1 nM Bind
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1
CHEMBL4476784 drd3_human Human Yes 8.9 EC50 = 1.2 nM Bind
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4100634 drd3_human Human No 8.9 EC50 = 1.2 nM Funct
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
370 7 1 2 6.5 CCCCCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21
CHEMBL27254 drd3_chlae Green monkey No 8.9 EC50 = 1.2 nM Funct
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
493 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)cc2)CC1
CHEMBL4466245 drd3_human Human No 8.9 EC50 = 1.2 nM Funct
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
389 9 3 6 4.1 CCCN(CCCCCc1cc(O)ccc1O)[C@H]1CCc2nc(N)sc2C1
CHEMBL556269 drd3_human Human No 8.9 EC50 = 1.2 nM Funct
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
460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1
CHEMBL273273 drd3_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC
CHEMBL2152633 drd3_human Human No 8.9 EC50 = 1.3 nM Funct
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
438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL240773 drd3_human Human Yes 8.9 EC50 = 1.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL4081780 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL240773 drd3_human Human Yes 8.9 EC50 = 1.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL142020 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1
CHEMBL3740041 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
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
472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3742426 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
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
472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL484598 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
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
286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O
CHEMBL4081780 drd3_human Human No 8.9 EC50 = 1.4 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL2146499 drd3_human Human No 8.8 EC50 = 1.5 nM Funct
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
511 9 2 7 4.3 CCCN(CC[C@H]1CC[C@H](NS(=O)(=O)c2cccnc2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL301265 drd3_human Human Yes 8.8 EC50 = 1.5 nM Bind
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL301265 drd3_human Human Yes 8.8 EC50 = 1.5 nM Funct
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL301265 drd3_human Human Yes 8.8 EC50 = 1.5 nM Bind
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL124444 drd3_human Human No 8.8 EC50 = 1.5 nM Funct
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1
CHEMBL514885 drd3_human Human No 8.8 EC50 = 1.5 nM Funct
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
475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL599636 drd3_human Human No 8.8 EC50 = 1.6 nM Funct
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
460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2c(O)cccc2C1
CHEMBL484358 drd3_human Human No 8.8 EC50 = 1.6 nM Bind
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1
CHEMBL4098174 drd3_human Human No 8.8 EC50 = 1.7 nM Funct
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
527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1
CHEMBL2203406 drd3_human Human No 8.8 EC50 = 1.7 nM Funct
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
478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1
CHEMBL240773 drd3_rat Rat Yes 8.8 EC50 = 1.7 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL240773 drd3_human Human Yes 8.8 EC50 = 1.7 nM Bind
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL59 drd3_human Human Yes 8.7 EC50 = 1.8 nM Bind
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.7 EC50 = 1.8 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL25236 drd3_human Human Yes 8.7 EC50 = 1.8 nM Funct
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
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL25236 drd3_human Human Yes 8.7 EC50 = 1.8 nM Funct
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL3287397 drd3_human Human No 8.7 EC50 = 1.9 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287397 drd3_human Human No 8.7 EC50 = 1.9 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL240773 drd3_human Human Yes 8.0 EC50 = 10 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL465 drd3_human Human Yes 8.0 EC50 = 10.2 nM Funct
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
314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C
CHEMBL589 drd3_human Human Yes 8.0 EC50 = 10.3 nM Funct
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
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL589 drd3_human Human Yes 8.0 EC50 = 10.3 nM Funct
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
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL3798334 drd3_human Human No 8.0 EC50 = 10.5 nM Funct
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
419 7 1 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL59 drd3_human Human Yes 8.0 EC50 = 10.6 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL3740778 drd3_human Human No 8.0 EC50 = 10.9 nM Funct
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
469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3742429 drd3_human Human No 8.0 EC50 = 10.9 nM Funct
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
469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3262809 drd3_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
374 6 0 4 3.2 COc1ccc(C(=O)N2CCN(CCOc3ccc(Cl)cc3)CC2)cc1
CHEMBL4586582 drd3_human Human Yes 6.0 EC50 = 1000.2 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4596341 drd3_human Human Yes 6.0 EC50 = 1000.2 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4581907 drd3_human Human Yes 7.0 EC50 = 105 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
427 5 1 3 3.8 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Br)cc2)CC1
CHEMBL4102620 drd3_human Human No 7.0 EC50 = 109.7 nM Funct
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
532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1
CHEMBL3590083 drd3_human Human No 8.0 EC50 = 11 nM Funct
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
432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1
CHEMBL4060896 drd3_human Human No 8.0 EC50 = 11 nM Funct
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
540 9 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2)c1
CHEMBL3797771 drd3_human Human No 8.0 EC50 = 11.2 nM Funct
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
487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12
CHEMBL3800680 drd3_human Human No 8.0 EC50 = 11.2 nM Funct
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
487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12
CHEMBL3799465 drd3_human Human No 7.9 EC50 = 11.4 nM Funct
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
477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12
CHEMBL3800684 drd3_human Human No 7.9 EC50 = 11.4 nM Funct
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
477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12
CHEMBL3799626 drd3_human Human No 7.9 EC50 = 11.9 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL3287399 drd3_human Human No 7.0 EC50 = 110 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CN3C(=C(C=N3)C=O)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4102620 drd3_human Human No 7.0 EC50 = 110 nM Funct
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
532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1
CHEMBL210461 drd3_human Human No 7.0 EC50 = 110 nM Funct
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
535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2
CHEMBL4522558 drd3_human Human Yes 5.0 EC50 = 11086 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4597048 drd3_human Human Yes 5.0 EC50 = 11086 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL3287399 drd3_human Human No 7.0 EC50 = 112.2 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CN3C(=C(C=N3)C=O)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3590083 drd3_human Human No 6.9 EC50 = 114 nM Funct
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
432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1
CHEMBL4462053 drd3_human Human No 6.9 EC50 = 114 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
397 5 1 3 4.0 Cc1cc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)ccc1Cl
CHEMBL4574586 drd3_human Human No 6.9 EC50 = 114 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
383 5 1 3 3.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Cl)cc2)CC1
CHEMBL3800633 drd3_human Human No 6.9 EC50 = 115 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
418 7 2 5 3.1 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)[C@@H]3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3262808 drd3_human Human Yes 6.9 EC50 = 115 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
340 6 0 4 2.5 COc1ccc(C(=O)N2CCN(CCOc3ccccc3)CC2)cc1
CHEMBL4514438 drd3_human Human No 6.9 EC50 = 116 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
355 6 0 5 2.2 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)c(C)c1
CHEMBL4525545 drd3_human Human No 6.9 EC50 = 118 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
300 5 1 4 1.2 O=C(c1ccc[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL3287405 drd3_human Human No 7.9 EC50 = 12 nM Funct
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
443 7 0 6 4.5 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4071121 drd3_human Human No 7.9 EC50 = 12 nM Funct
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
472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1
CHEMBL3287405 drd3_human Human No 7.9 EC50 = 12.3 nM Funct
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
443 7 0 6 4.5 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4443039 drd3_human Human No 7.9 EC50 = 12.5 nM Funct
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
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL4595150 drd3_human Human No 7.9 EC50 = 12.5 nM Funct
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
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL4072140 drd3_human Human No 6.9 EC50 = 120 nM Funct
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
510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4059573 drd3_human Human No 5.9 EC50 = 1200 nM Funct
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
497 8 1 4 6.1 O=C(NCCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL3799626 drd3_human Human No 6.9 EC50 = 125 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL4456795 drd3_human Human No 6.9 EC50 = 126 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
367 5 1 3 3.1 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(F)cc2)CC1
CHEMBL4475406 drd3_human Human Yes 6.9 EC50 = 126.4 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC
CHEMBL4597530 drd3_human Human Yes 6.9 EC50 = 126.4 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC
CHEMBL4551448 drd3_human Human No 7.9 EC50 = 13 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 1 4 2.7 Cc1ccc2[nH]c(C(=O)N3CCN(CCOc4cccnc4)CC3)cc2c1
CHEMBL3597636 drd3_human Human No 7.9 EC50 = 13 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1
CHEMBL287198 drd3_human Human No 7.9 EC50 = 13 nM Funct
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12
CHEMBL4470996 drd3_human Human No 7.9 EC50 = 13.3 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
367 5 0 5 3.1 O=C(c1cc2ccccc2s1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4447103 drd3_human Human No 7.9 EC50 = 13.5 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1cc2cccnc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4470213 drd3_human Human No 6.9 EC50 = 130 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(C)cc4[nH]3)CC2)cc1
CHEMBL4087889 drd3_human Human No 6.9 EC50 = 130 nM Funct
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
443 8 1 4 5.4 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1
CHEMBL4518079 drd3_human Human No 5.9 EC50 = 1300 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
394 6 1 5 2.9 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc([N+](=O)[O-])cc2)CC1
CHEMBL398480 drd3_human Human No 5.9 EC50 = 1312 nM Funct
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
219 3 1 3 2.0 C=CCN1CCOC(c2cccc(O)c2)C1
CHEMBL4070196 drd3_human Human No 7.9 EC50 = 14 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL4092052 drd3_human Human No 7.9 EC50 = 14 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4099798 drd3_human Human No 7.9 EC50 = 14 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL4095588 drd3_human Human No 7.9 EC50 = 14 nM Funct
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
445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1
CHEMBL4116454 drd3_human Human No 7.9 EC50 = 14 nM Funct
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
445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1
CHEMBL3798372 drd3_human Human No 7.9 EC50 = 14.1 nM Funct
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
479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2
CHEMBL3800683 drd3_human Human No 7.9 EC50 = 14.1 nM Funct
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
479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2
CHEMBL4092052 drd3_human Human No 7.9 EC50 = 14.1 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL3800489 drd3_human Human No 7.8 EC50 = 14.4 nM Funct
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
433 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL3597643 drd3_human Human No 6.9 EC50 = 140 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1
CHEMBL4290759 drd3_human Human No 5.9 EC50 = 1400 nM Funct
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
379 7 2 5 2.8 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(C#N)cc1)CC2
CHEMBL4586582 drd3_human Human Yes 6.8 EC50 = 142.8 nM Funct
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
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4596341 drd3_human Human Yes 6.8 EC50 = 142.8 nM Funct
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
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL3800165 drd3_human Human No 5.9 EC50 = 1423 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
273 5 1 4 2.1 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1
CHEMBL3797740 drd3_human Human No 6.8 EC50 = 148 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
245 3 1 3 1.6 CCCN(C)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL3287404 drd3_human Human No 7.8 EC50 = 15 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4069565 drd3_human Human No 7.8 EC50 = 15 nM Funct
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
558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL3287404 drd3_human Human No 7.8 EC50 = 15.1 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4069565 drd3_human Human No 7.8 EC50 = 15.1 nM Funct
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
558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL4092900 drd3_human Human No 6.8 EC50 = 150 nM Funct
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
496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4079093 drd3_human Human No 5.8 EC50 = 1500 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4117318 drd3_human Human No 5.8 EC50 = 1500 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4461237 drd3_human Human Yes 6.8 EC50 = 151 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
363 5 1 3 3.3 Cc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4079093 drd3_human Human No 5.8 EC50 = 1513.6 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4117318 drd3_human Human No 5.8 EC50 = 1513.6 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL26188 drd3_human Human No 6.8 EC50 = 154.9 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1
CHEMBL4540693 drd3_human Human No 6.8 EC50 = 155 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(OC)cc4[nH]3)CC2)cc1
CHEMBL3597637 drd3_human Human No 7.8 EC50 = 16 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1
CHEMBL4474192 drd3_human Human No 6.8 EC50 = 160 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4c(Cl)cccc4[nH]3)CC2)cc1
CHEMBL4585248 drd3_human Human No 6.8 EC50 = 160 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 7 0 5 2.9 COc1ccc(OC(C)CN2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1
CHEMBL4435184 drd3_human Human No 5.8 EC50 = 1600 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
377 6 1 3 3.6 CCc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4454068 drd3_human Human Yes 5.8 EC50 = 1601 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1
CHEMBL4083252 drd3_human Human No 6.8 EC50 = 166.7 nM Bind
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1
CHEMBL4471655 drd3_human Human No 6.8 EC50 = 167 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4cccnc4[nH]3)CC2)cc1
CHEMBL4476784 drd3_human Human Yes 7.8 EC50 = 17 nM Bind
Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4563661 drd3_human Human No 7.8 EC50 = 17 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
341 6 0 5 1.9 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)cc1
CHEMBL4103339 drd3_human Human No 7.8 EC50 = 17 nM Funct
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
483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4441358 drd3_human Human No 7.8 EC50 = 17.9 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl
CHEMBL304605 drd3_human Human No 6.8 EC50 = 173 nM Funct
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
491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2
CHEMBL304605 drd3_human Human No 6.8 EC50 = 173 nM Funct
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
491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2
CHEMBL4454380 drd3_human Human Yes 6.8 EC50 = 177.5 nM Funct
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
482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL4596929 drd3_human Human Yes 6.8 EC50 = 177.5 nM Funct
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
482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL3799157 drd3_human Human No 6.8 EC50 = 178 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
245 3 1 4 1.4 CCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2
CHEMBL4060461 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(C=NN4C=C3)/C=N/O
CHEMBL4079093 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4117318 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL209876 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1
CHEMBL4079093 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4117318 drd3_human Human No 7.8 EC50 = 18 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4060461 drd3_human Human No 7.7 EC50 = 18.2 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(C=NN4C=C3)/C=N/O
CHEMBL434665 drd3_human Human Yes 7.7 EC50 = 18.3 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
231 3 2 3 1.3 CCCN[C@@H]1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL4069565 drd3_human Human No 7.7 EC50 = 18.6 nM Funct
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
558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL4067439 drd3_human Human No 7.7 EC50 = 18.6 nM Funct
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
408 9 0 7 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=C(C=N4)C=O)C=C3
CHEMBL277301 drd3_human Human No 5.7 EC50 = 1819.7 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@@H](c3ccccc3)CC2)CC1
CHEMBL419792 drd3_human Human Yes 6.7 EC50 = 186 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3
CHEMBL240773 drd3_human Human Yes 6.7 EC50 = 186.3 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL3799271 drd3_human Human Yes 5.7 EC50 = 1890 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
189 0 2 3 0.2 N[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL4067439 drd3_human Human No 7.7 EC50 = 19 nM Funct
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
408 9 0 7 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=C(C=N4)C=O)C=C3
CHEMBL4063235 drd3_human Human No 7.7 EC50 = 19 nM Funct
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
405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1
CHEMBL4081780 drd3_human Human No 7.7 EC50 = 19 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL4063235 drd3_human Human No 7.7 EC50 = 19.1 nM Funct
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
405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1
CHEMBL3798943 drd3_human Human No 7.7 EC50 = 19.2 nM Funct
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
403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL3800677 drd3_human Human No 7.7 EC50 = 19.2 nM Funct
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
403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL589 drd3_human Human Yes 7.7 EC50 = 19.2 nM Funct
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
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL1112 drd3_human Human Yes 7.7 EC50 = 19.5 nM Funct
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
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL1112 drd3_human Human Yes 7.7 EC50 = 19.5 nM Funct
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
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL3800633 drd3_human Human No 7.7 EC50 = 19.6 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
418 7 2 5 3.1 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)[C@@H]3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL4065510 drd3_human Human No 7.7 EC50 = 20.0 nM Funct
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
538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4471482 drd3_human Human No 5.7 EC50 = 1900 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
392 6 1 4 3.1 COc1ccc(N(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4562300 drd3_human Human No 5.7 EC50 = 1900 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3[nH]c4ccccc4c3C)CC2)cc1
CHEMBL4443579 drd3_human Human No 6.7 EC50 = 192 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)cc1
CHEMBL4517102 drd3_human Human No 6.7 EC50 = 196 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl
CHEMBL394292 drd3_human Human No 8.7 EC50 = 2 nM Funct
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
429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1
CHEMBL364516 drd3_human Human No 8.7 EC50 = 2 nM Funct
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
None None None None
CHEMBL59 drd3_human Human Yes 8.7 EC50 = 2.1 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL241212 drd3_human Human No 8.7 EC50 = 2.1 nM Funct
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
391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1
CHEMBL4100735 drd3_human Human No 8.7 EC50 = 2.1 nM Funct
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
458 8 2 5 3.8 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4ccccc4)CC3)c2)c1
CHEMBL484358 drd3_human Human No 8.7 EC50 = 2.1 nM Funct
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
414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1
CHEMBL240773 drd3_human Human Yes 8.7 EC50 = 2.1 nM Bind
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL194493 drd3_human Human No 8.7 EC50 = 2.2 nM Funct
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
448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1
CHEMBL484599 drd3_human Human No 8.6 EC50 = 2.3 nM Funct
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
274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21
CHEMBL485128 drd3_human Human No 8.6 EC50 = 2.3 nM Funct
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
287 2 0 4 2.5 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)COC4=O
CHEMBL4099798 drd3_human Human No 8.6 EC50 = 2.3 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL59 drd3_human Human Yes 8.6 EC50 = 2.3 nM Bind
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL1771109 drd3_human Human No 8.6 EC50 = 2.3 nM Funct
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
459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1
CHEMBL4099798 drd3_human Human No 8.6 EC50 = 2.3 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1
CHEMBL240773 drd3_human Human Yes 8.6 EC50 = 2.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL372020 drd3_human Human No 8.6 EC50 = 2.4 nM Bind
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1
CHEMBL4451683 drd3_human Human No 8.6 EC50 = 2.6 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl
CHEMBL3590081 drd3_human Human No 8.6 EC50 = 2.6 nM Funct
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
396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1
CHEMBL4072282 drd3_human Human No 8.6 EC50 = 2.6 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL240773 drd3_human Human Yes 8.6 EC50 = 2.6 nM Bind
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL240773 drd3_human Human Yes 8.6 EC50 = 2.6 nM Bind
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL240773 drd3_human Human Yes 8.6 EC50 = 2.6 nM Bind
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL240773 drd3_human Human Yes 8.6 EC50 = 2.6 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL484202 drd3_human Human No 8.6 EC50 = 2.6 nM Bind
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1
CHEMBL4457171 drd3_human Human No 8.6 EC50 = 2.6 nM Funct
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
389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1
CHEMBL4072282 drd3_human Human No 8.6 EC50 = 2.6 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL59 drd3_human Human Yes 8.6 EC50 = 2.7 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL25236 drd3_human Human Yes 8.6 EC50 = 2.7 nM Funct
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
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL1771110 drd3_human Human No 8.6 EC50 = 2.8 nM Funct
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
475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1
CHEMBL310867 drd3_human Human Yes 8.6 EC50 = 2.8 nM Funct
Effective concentration required for agonistic activity against human Dopamine receptor D3Effective concentration required for agonistic activity against human Dopamine receptor D3
271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1
CHEMBL59 drd3_human Human Yes 8.5 EC50 = 2.9 nM Bind
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL240773 drd3_human Human Yes 8.5 EC50 = 2.9 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL1112 drd3_human Human Yes 7.7 EC50 = 20 nM Funct
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
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL3597635 drd3_human Human No 7.7 EC50 = 20 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
438 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1
CHEMBL1112 drd3_human Human Yes 7.7 EC50 = 20 nM Funct
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
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL4065510 drd3_human Human No 7.7 EC50 = 20 nM Funct
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
538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL246439 drd3_human Human Yes 7.7 EC50 = 20.2 nM Funct
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
354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1
CHEMBL4573578 drd3_human Human No 7.7 EC50 = 20.4 nM Funct
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
401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3798010 drd3_human Human No 7.7 EC50 = 20.6 nM Funct
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
475 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)OC1CCCc2ccccc21
CHEMBL4587874 drd3_human Human No 6.7 EC50 = 200 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1cc2ncccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4472813 drd3_human Human No 6.7 EC50 = 208 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)cc1
CHEMBL114541 drd3_human Human No 6.7 EC50 = 208.9 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
405 7 1 3 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1
CHEMBL4476784 drd3_human Human Yes 7.7 EC50 = 21 nM Bind
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL3799147 drd3_human Human No 7.7 EC50 = 21.7 nM Funct
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
417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL3800675 drd3_human Human No 7.7 EC50 = 21.7 nM Funct
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
417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1
CHEMBL1744080 drd3_human Human Yes 7.7 EC50 = 21.8 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
273 5 1 4 2.8 CCCN(CCC)[C@@H]1Cc2cccc3nc(O)n(c23)C1
CHEMBL26181 drd3_human Human Yes 7.7 EC50 = 21.8 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
273 5 1 4 2.8 CCCN(CCC)[C@@H]1Cc2cccc3nc(O)n(c23)C1
CHEMBL4533633 drd3_human Human No 6.7 EC50 = 210 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3c[nH]c4ccccc34)CC2)cc1
CHEMBL4526466 drd3_human Human No 5.7 EC50 = 2100 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
371 7 0 6 1.9 COc1ccc(OCCN2CCN(C(=O)c3ccc(OC)cn3)CC2)cc1
CHEMBL4098174 drd3_human Human No 6.7 EC50 = 218.8 nM Funct
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
527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1
CHEMBL3798803 drd3_human Human No 7.7 EC50 = 22 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
259 4 1 4 1.7 CCCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2
CHEMBL1627316 drd3_human Human No 7.6 EC50 = 22.8 nM Funct
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
461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1
CHEMBL4098174 drd3_human Human No 6.7 EC50 = 220 nM Funct
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
527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1
CHEMBL4474673 drd3_human Human No 4.7 EC50 = 22000 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
341 6 0 5 1.9 COc1ccc(OCCN2CCN(C(=O)c3ccncc3)CC2)cc1
CHEMBL4466748 drd3_human Human No 6.7 EC50 = 225 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(Cl)cc4[nH]3)CC2)cc1
CHEMBL4785109 drd3_human Human No 7.6 EC50 = 23 nM Funct
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
427 7 1 4 4.8 O=C(NC/C=C/CN1CCN(c2ccccc2)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4071121 drd3_human Human No 5.6 EC50 = 2300 nM Funct
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
472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1
CHEMBL397770 drd3_human Human Yes 6.6 EC50 = 232 nM Funct
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
374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1
CHEMBL4071121 drd3_human Human No 5.6 EC50 = 2344.2 nM Funct
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
472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1
CHEMBL180060 drd3_human Human No 7.6 EC50 = 24.1 nM Funct
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
529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1
CHEMBL4063681 drd3_human Human No 6.6 EC50 = 240 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1
CHEMBL4117347 drd3_human Human No 6.6 EC50 = 240 nM Funct
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
497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1
CHEMBL246438 drd3_human Human No 6.6 EC50 = 248 nM Funct
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
354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1
CHEMBL240773 drd3_human Human Yes 7.6 EC50 = 25.1 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL3798841 drd3_human Human No 7.6 EC50 = 25.4 nM Funct
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
501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12
CHEMBL3800679 drd3_human Human No 7.6 EC50 = 25.4 nM Funct
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
501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12
CHEMBL3798803 drd3_human Human No 7.6 EC50 = 25.6 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
259 4 1 4 1.7 CCCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2
CHEMBL4470786 drd3_human Human No 7.6 EC50 = 25.7 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 1 4 2.7 Cc1cccc2cc(C(=O)N3CCN(CCOc4cccnc4)CC3)[nH]c12
CHEMBL4526308 drd3_human Human Yes 5.6 EC50 = 2500 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
370 7 0 5 2.5 COc1ccc(OCCN2CCN(C(=O)c3ccccc3OC)CC2)cc1
CHEMBL4099711 drd3_human Human No 7.6 EC50 = 26.9 nM Funct
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
410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1
CHEMBL4436562 drd3_human Human No 5.6 EC50 = 2600 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
368 7 0 4 3.1 CCc1ccc(OCCN2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1
CHEMBL4460818 drd3_human Human No 6.6 EC50 = 266 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4c(C)cccc4[nH]3)CC2)cc1
CHEMBL4099711 drd3_human Human No 7.6 EC50 = 27 nM Funct
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
410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1
CHEMBL102463 drd3_human Human Yes 7.6 EC50 = 27 nM Funct
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
221 3 1 3 2.2 CCCN1CCOC(c2cccc(O)c2)C1
CHEMBL4442548 drd3_human Human Yes 5.6 EC50 = 2755 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1
CHEMBL4449219 drd3_human Human No 6.6 EC50 = 278 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
370 7 0 5 2.5 COc1ccc(C(=O)N2CCN(CCOc3ccccc3OC)CC2)cc1
CHEMBL442535 drd3_human Human No 7.6 EC50 = 28 nM Funct
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)cc(Br)c2ccccc12
CHEMBL4098803 drd3_human Human No 7.5 EC50 = 28.8 nM Funct
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
380 8 0 6 3.3 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=CC=N4)C=C3
CHEMBL4594046 drd3_human Human No 6.6 EC50 = 280 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1cccc(OCCN2CCN(C(=O)c3cc4cnccc4[nH]3)CC2)c1
CHEMBL4519354 drd3_human Human No 5.6 EC50 = 2800 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4ncccc4[nH]3)CC2)cc1
CHEMBL4592753 drd3_human Human No 5.6 EC50 = 2802 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1
CHEMBL4448833 drd3_human Human No 6.6 EC50 = 284 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1cccc(OCCN2CCN(C(=O)c3cc4cc(OC)ccc4[nH]3)CC2)c1
CHEMBL4471623 drd3_human Human No 6.5 EC50 = 285 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1cccc(OCCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c1
CHEMBL4098803 drd3_human Human No 7.5 EC50 = 29 nM Funct
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
380 8 0 6 3.3 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CN4C(=CC=N4)C=C3
CHEMBL4522558 drd3_human Human Yes 7.5 EC50 = 29.6 nM Funct
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
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4597048 drd3_human Human Yes 7.5 EC50 = 29.6 nM Funct
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
509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4578060 drd3_human Human No 6.5 EC50 = 290 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 5 1 5 2.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc3c(c2)OCO3)CC1
CHEMBL4545654 drd3_human Human No 5.5 EC50 = 2900 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)cc1
CHEMBL4455456 drd3_human Human No 8.5 EC50 = 3 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 5 1 4 3.1 O=C(c1cc2ccc(Cl)cc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL25236 drd3_chlae Green monkey Yes 8.5 EC50 = 3 nM Funct
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL25236 drd3_human Human Yes 8.5 EC50 = 3 nM Funct
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL484202 drd3_human Human No 8.5 EC50 = 3.1 nM Funct
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
438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1
CHEMBL240773 drd3_human Human Yes 8.5 EC50 = 3.1 nM Funct
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL1771107 drd3_human Human No 8.5 EC50 = 3.3 nM Funct
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
469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1
CHEMBL477250 drd3_human Human No 8.5 EC50 = 3.3 nM Funct
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
393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1
CHEMBL240773 drd3_human Human Yes 8.5 EC50 = 3.3 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL378455 drd3_human Human No 8.5 EC50 = 3.3 nM Funct
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
315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1
CHEMBL390253 drd3_human Human No 8.5 EC50 = 3.4 nM Funct
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
498 8 2 5 4.4 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL193337 drd3_human Human No 8.5 EC50 = 3.4 nM Bind
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1
CHEMBL240773 drd3_human Human Yes 8.5 EC50 = 3.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL3125987 drd3_human Human No 8.5 EC50 = 3.4 nM Funct
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
505 9 1 7 4.8 CCCN(CCN1CCN(c2ccc(-c3cccc(OC)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL59 drd3_human Human Yes 8.5 EC50 = 3.5 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL392437 drd3_human Human No 8.5 EC50 = 3.5 nM Funct
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
429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1
CHEMBL194555 drd3_human Human No 8.5 EC50 = 3.5 nM Funct
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
None None None None
CHEMBL4475406 drd3_human Human Yes 8.5 EC50 = 3.6 nM Funct
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
489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC
CHEMBL4597530 drd3_human Human Yes 8.5 EC50 = 3.6 nM Funct
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
489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC
CHEMBL4090581 drd3_human Human No 8.4 EC50 = 3.6 nM Funct
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
472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1
CHEMBL4090581 drd3_human Human No 8.4 EC50 = 3.6 nM Funct
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
472 9 2 5 4.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)cc2)c1
CHEMBL3797209 drd3_human Human No 8.4 EC50 = 3.7 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
315 7 0 4 3.3 CCCN1C2=CC=CC3=C2N(C1=O)C[C@@H](C3)N(CCC)CCC
CHEMBL4062484 drd3_human Human No 8.4 EC50 = 3.7 nM Funct
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
515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1
CHEMBL4073966 drd3_human Human No 8.4 EC50 = 3.7 nM Funct
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
472 9 2 5 4.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4ccccc4)CC3)c2)c1
CHEMBL4069091 drd3_human Human No 8.4 EC50 = 3.8 nM Funct
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
474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1
CHEMBL338606 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1
CHEMBL242434 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
540 9 1 6 4.9 CC(=O)OC(CCNC(=O)c1ccc(-c2ccccn2)cc1)CN1CCN(c2cccc(Cl)c2Cl)CC1
CHEMBL4102620 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1
CHEMBL191962 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
None None None None
CHEMBL3740286 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL3742427 drd3_human Human No 8.4 EC50 = 3.9 nM Funct
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
472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1
CHEMBL2387709 drd3_human Human No 7.5 EC50 = 30.3 nM Funct
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
392 7 1 4 3.7 CCCN(CCN1CCN(c2ccccc2)CC1)[C@@H]1CCc2ccc(N)cc2C1
CHEMBL3797740 drd3_human Human No 7.5 EC50 = 30.7 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 3 1.6 CCCN(C)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL4079301 drd3_human Human No 7.5 EC50 = 30.9 nM Funct
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
405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1
CHEMBL4079301 drd3_human Human No 7.5 EC50 = 31 nM Funct
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
405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1
CHEMBL302374 drd3_human Human No 7.5 EC50 = 31.7 nM Funct
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
531 7 1 3 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1
CHEMBL4450129 drd3_human Human No 6.5 EC50 = 310 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 6 0 6 2.3 COc1ccc(C(=O)N2CCN(CCOc3ccc4c(c3)OCO4)CC2)cc1
CHEMBL4530116 drd3_human Human No 6.5 EC50 = 310 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 0 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4n3C)CC2)cc1
CHEMBL4522471 drd3_human Human No 7.5 EC50 = 32 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
397 5 1 3 4.0 CC(CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)Oc1ccc(Cl)cc1
CHEMBL250003 drd3_human Human No 7.5 EC50 = 32 nM Funct
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
237 3 2 4 1.9 CCCN1CCO[C@H](c2cc(O)cc(O)c2)C1
CHEMBL2180638 drd3_human Human No 7.5 EC50 = 32.2 nM Funct
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
295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1
CHEMBL4099236 drd3_human Human No 6.5 EC50 = 320 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4116199 drd3_human Human No 6.5 EC50 = 320 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL59 drd3_human Human Yes 7.5 EC50 = 33 nM Bind
Agonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4518951 drd3_human Human No 7.5 EC50 = 33 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 5 1 4 3.1 O=C(c1cc2cccc(Cl)c2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4566746 drd3_human Human No 7.5 EC50 = 33 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1nc2ccccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4472566 drd3_human Human No 7.5 EC50 = 33.8 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
379 6 1 4 3.0 COc1cccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c1
CHEMBL4068218 drd3_human Human No 6.5 EC50 = 330 nM Funct
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
459 9 1 5 5.1 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1
CHEMBL4117124 drd3_human Human No 6.5 EC50 = 330 nM Funct
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
459 9 1 5 5.1 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1
CHEMBL4472861 drd3_human Human Yes 5.5 EC50 = 3300 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
396 6 0 5 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4s3)CC2)cc1
CHEMBL4062484 drd3_human Human No 6.5 EC50 = 338.8 nM Funct
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
515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1
CHEMBL4062484 drd3_human Human No 6.5 EC50 = 340 nM Funct
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
515 8 1 4 6.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)c(F)c1
CHEMBL3799271 drd3_human Human Yes 5.5 EC50 = 3400 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
189 0 2 3 0.2 N[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1
CHEMBL246020 drd3_human Human No 6.5 EC50 = 347 nM Funct
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
338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1
CHEMBL240773 drd3_human Human Yes 7.5 EC50 = 35 nM Bind
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL401157 drd3_human Human No 7.5 EC50 = 35 nM Funct
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
239 3 1 3 2.3 CCCN1CCOC(c2ccc(F)c(O)c2)C1
CHEMBL4522768 drd3_human Human No 5.5 EC50 = 3500 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
350 5 1 4 2.4 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccccn2)CC1
CHEMBL250002 drd3_human Human No 7.4 EC50 = 36 nM Funct
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
239 3 1 3 2.3 CCCN1CCO[C@H](c2ccc(F)c(O)c2)C1
CHEMBL98836 drd3_rat Rat No 7.4 EC50 = 36 nM Funct
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
265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21
CHEMBL4293886 drd3_human Human No 6.4 EC50 = 360 nM Funct
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
384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1
CHEMBL4060403 drd3_human Human No 7.4 EC50 = 37 nM Funct
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
459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12
CHEMBL399892 drd3_human Human Yes 7.4 EC50 = 37 nM Funct
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
237 3 2 4 1.9 CCCN1CCOC(c2cc(O)cc(O)c2)C1
CHEMBL4090459 drd3_human Human No 7.4 EC50 = 37 nM Funct
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
489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1
CHEMBL4548340 drd3_human Human No 7.4 EC50 = 37.6 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 0 5 2.4 Cn1c(C(=O)N2CCN(CCOc3cccnc3)CC2)cc2ccccc21
CHEMBL3799311 drd3_human Human No 7.4 EC50 = 37.7 nM Funct
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
489 7 1 4 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(F)c2ccccc12
CHEMBL3800678 drd3_human Human No 7.4 EC50 = 37.7 nM Funct
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
489 7 1 4 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(F)c2ccccc12
CHEMBL4065510 drd3_human Human No 7.4 EC50 = 37.8 nM Funct
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
538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4065510 drd3_human Human No 7.4 EC50 = 37.8 nM Funct
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
538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4072140 drd3_human Human No 6.4 EC50 = 370 nM Funct
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
510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4072140 drd3_human Human No 6.4 EC50 = 371.5 nM Funct
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
510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4476784 drd3_human Human Yes 7.4 EC50 = 38 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4096353 drd3_human Human No 7.4 EC50 = 38 nM Funct
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
436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1
CHEMBL3287403 drd3_human Human No 7.4 EC50 = 38.9 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4092900 drd3_human Human No 6.4 EC50 = 380 nM Funct
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
496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4092900 drd3_human Human No 6.4 EC50 = 380.2 nM Funct
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
496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12
CHEMBL4471346 drd3_human Human No 5.4 EC50 = 3800 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
433 6 1 4 3.9 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(OC(F)(F)F)cc2)CC1
CHEMBL3287403 drd3_human Human No 7.4 EC50 = 39 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL589 drd3_human Human Yes 8.4 EC50 = 4 nM Funct
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
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL4094794 drd3_human Human No 8.4 EC50 = 4 nM Funct
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
486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4459426 drd3_human Human No 8.4 EC50 = 4.3 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 1 4 2.7 Cc1ccc2cc(C(=O)N3CCN(CCOc4cccnc4)CC3)[nH]c2c1
CHEMBL2146503 drd3_human Human No 8.4 EC50 = 4.3 nM Funct
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
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
CHEMBL4472628 drd3_human Human No 8.4 EC50 = 4.4 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 5 1 4 3.1 O=C(c1cc2c(Cl)cccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4078351 drd3_human Human No 8.4 EC50 = 4.4 nM Funct
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
570 10 2 6 5.5 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1cccc(C(N)=O)c1
CHEMBL162762 drd3_human Human Yes 8.4 EC50 = 4.4 nM Bind
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1
CHEMBL194099 drd3_human Human No 8.4 EC50 = 4.5 nM Bind
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1
CHEMBL484732 drd3_human Human No 8.3 EC50 = 4.7 nM Funct
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
300 2 1 3 2.1 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CCNC4=O
CHEMBL4544583 drd3_human Human No 8.3 EC50 = 4.7 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl
CHEMBL59 drd3_human Human Yes 8.3 EC50 = 4.8 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.3 EC50 = 4.8 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL370713 drd3_human Human No 8.3 EC50 = 4.8 nM Funct
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
433 7 1 4 4.1 COc1ccc(C(=O)NC/C=C/CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1
CHEMBL249793 drd3_human Human Yes 7.4 EC50 = 40 nM Funct
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
236 3 2 4 1.8 CCCN1CCOC(c2ccc(O)c(N)c2)C1
CHEMBL4060461 drd3_human Human No 7.4 EC50 = 40.7 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(C=NN4C=C3)/C=N/O
CHEMBL3287406 drd3_human Human No 7.4 EC50 = 40.7 nM Funct
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
443 7 0 6 4.5 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4445988 drd3_human Human No 7.4 EC50 = 41 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c(Cl)c1
CHEMBL4060461 drd3_human Human No 7.4 EC50 = 41 nM Funct
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
423 9 1 8 3.1 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(C=NN4C=C3)/C=N/O
CHEMBL3287392 drd3_human Human No 7.4 EC50 = 41 nM Funct
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
418 7 0 5 4.6 C1CN(CCN1CCCCOC2=CN3C(=CC=N3)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287406 drd3_human Human No 7.4 EC50 = 41 nM Funct
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
443 7 0 6 4.5 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL246637 drd3_human Human Yes 7.4 EC50 = 41.5 nM Funct
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
374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1
CHEMBL3287392 drd3_human Human No 7.4 EC50 = 41.7 nM Funct
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
418 7 0 5 4.6 C1CN(CCN1CCCCOC2=CN3C(=CC=N3)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4476699 drd3_human Human No 6.4 EC50 = 410 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl
CHEMBL4440776 drd3_human Human No 6.4 EC50 = 411 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4c(OC)cccc4[nH]3)CC2)cc1
CHEMBL4473910 drd3_human Human No 7.4 EC50 = 42 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 0 5 2.7 O=C(c1cc2ccccc2o1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4070091 drd3_human Human No 7.4 EC50 = 42 nM Funct
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
418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1
CHEMBL396024 drd3_human Human No 7.4 EC50 = 42 nM Funct
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
509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2
CHEMBL3287403 drd3_human Human No 7.4 EC50 = 42 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287403 drd3_human Human No 7.4 EC50 = 42.7 nM Funct
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
461 8 1 7 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)/C=N/O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4294279 drd3_human Human No 6.4 EC50 = 420 nM Funct
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
370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2
CHEMBL249357 drd3_human Human No 6.4 EC50 = 427 nM Funct
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
264 4 2 4 1.3 CCCN1CCOC(c2ccc(O)c(C(N)=O)c2)C1
CHEMBL4577889 drd3_human Human Yes 6.4 EC50 = 430 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 0 5 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4o3)CC2)cc1
CHEMBL4438465 drd3_human Human No 5.4 EC50 = 4400 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 7 0 5 2.9 COc1ccc(OCCN2CCN(C(=O)c3ccc(OC)cc3)CC2C)cc1
CHEMBL4538239 drd3_human Human No 7.4 EC50 = 45 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1n[nH]c2ccccc12)N1CCN(CCOc2cccnc2)CC1
CHEMBL4091155 drd3_human Human No 7.4 EC50 = 45 nM Funct
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
431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1
CHEMBL2158640 drd3_human Human No 7.3 EC50 = 46 nM Funct
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
353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21
CHEMBL2221044 drd3_human Human No 7.3 EC50 = 46 nM Funct
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
353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21
CHEMBL4483569 drd3_human Human No 7.3 EC50 = 46 nM Bind
Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-induced mitogenesisAgonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-induced mitogenesis
454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl
CHEMBL4585651 drd3_human Human No 6.3 EC50 = 472 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
350 5 1 4 2.4 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccncc2)CC1
CHEMBL4542423 drd3_human Human No 6.3 EC50 = 473 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4cccc(C)c4[nH]3)CC2)cc1
CHEMBL110365 drd3_human Human No 7.3 EC50 = 49.0 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1
CHEMBL4294577 drd3_human Human No 6.3 EC50 = 490 nM Funct
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
372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2
CHEMBL4554045 drd3_human Human No 8.3 EC50 = 5 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 5 1 4 3.1 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2cncc(Cl)c2)CC1
CHEMBL3287402 drd3_human Human No 8.3 EC50 = 5 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)C=O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287402 drd3_human Human No 8.3 EC50 = 5.0 nM Funct
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
446 8 0 6 4.4 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)C=O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL240773 drd3_human Human Yes 8.3 EC50 = 5.2 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL1188090 drd3_human Human Yes 8.3 EC50 = 5.3 nM Funct
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
283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1
CHEMBL545783 drd3_human Human Yes 8.3 EC50 = 5.3 nM Funct
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
283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1
CHEMBL59 drd3_human Human Yes 8.3 EC50 = 5.3 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL301265 drd3_human Human Yes 8.3 EC50 = 5.4 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N
CHEMBL2028019 drd3_human Human No 8.2 EC50 = 5.8 nM Funct
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
426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL59 drd3_human Human Yes 8.2 EC50 = 5.8 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL2028019 drd3_human Human No 8.2 EC50 = 5.8 nM Funct
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
426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL3287396 drd3_human Human No 8.2 EC50 = 5.9 nM Funct
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
448 8 1 6 4.1 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)CO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287396 drd3_human Human No 8.2 EC50 = 5.9 nM Funct
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
448 8 1 6 4.1 C1CN(CCN1CCCCOC2=CC3=CC(=NN3C=C2)CO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4567332 drd3_human Human No 7.3 EC50 = 50 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1cccc(OCCN2CCN(C(=O)c3cc4cccnc4[nH]3)CC2)c1
CHEMBL4072821 drd3_human Human No 7.3 EC50 = 50 nM Funct
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
452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1
CHEMBL4072821 drd3_human Human No 7.3 EC50 = 50.1 nM Funct
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
452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1
CHEMBL1765634 drd3_human Human No 7.3 EC50 = 51 nM Funct
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
430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@@H]1CCn2nccc2C1
CHEMBL7549 drd3_human Human Yes 7.3 EC50 = 51.9 nM Funct
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
219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1
CHEMBL3797209 drd3_human Human No 7.3 EC50 = 51.9 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
315 7 0 4 3.3 CCCN1C2=CC=CC3=C2N(C1=O)C[C@@H](C3)N(CCC)CCC
CHEMBL4461742 drd3_human Human No 6.3 EC50 = 510 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 7 0 5 2.9 COc1ccc(OCCN2CCN(C(=O)c3ccc(OC)cc3)C(C)C2)cc1
CHEMBL4094794 drd3_human Human No 7.3 EC50 = 52 nM Funct
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
486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4094794 drd3_human Human No 7.3 EC50 = 52.5 nM Funct
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
486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4476784 drd3_human Human Yes 6.3 EC50 = 520 nM Bind
Agonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL4589125 drd3_human Human No 6.3 EC50 = 520 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4cc(OC)ccc4[nH]3)CC2)cc1
CHEMBL39 drd3_human Human Yes 6.3 EC50 = 523 nM Bind
Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligandBasal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL3798179 drd3_human Human No 7.3 EC50 = 53 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
417 7 3 4 2.9 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)[C@@H]3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3799157 drd3_human Human No 7.3 EC50 = 53.7 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 4 1.4 CCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2
CHEMBL4451542 drd3_human Human Yes 6.3 EC50 = 530 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
368 7 0 4 3.1 CCc1ccc(C(=O)N2CCN(CCOc3ccc(OC)cc3)CC2)cc1
CHEMBL251215 drd3_human Human No 6.3 EC50 = 547 nM Funct
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
207 2 1 3 1.8 CCN1CCOC(c2cccc(O)c2)C1
CHEMBL4471690 drd3_human Human Yes 6.3 EC50 = 548 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
340 6 0 4 2.5 COc1ccc(OCCN2CCN(C(=O)c3ccccc3)CC2)cc1
CHEMBL59 drd3_human Human Yes 7.3 EC50 = 55 nM Bind
Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4577943 drd3_human Human Yes 6.3 EC50 = 550 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
370 7 0 5 2.5 COc1ccc(OCCN2CCN(C(=O)c3cccc(OC)c3)CC2)cc1
CHEMBL4443054 drd3_human Human Yes 5.3 EC50 = 5581 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1
CHEMBL4080762 drd3_human Human No 7.3 EC50 = 56 nM Funct
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
380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1
CHEMBL3800165 drd3_human Human No 7.3 EC50 = 56.1 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
273 5 1 4 2.1 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1
CHEMBL4080762 drd3_human Human No 7.3 EC50 = 56.2 nM Funct
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
380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1
CHEMBL3287395 drd3_human Human No 7.3 EC50 = 56.2 nM Funct
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
490 9 0 7 4.8 CCOC(=O)C1=NN2C=CC(=CC2=C1)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL4587372 drd3_human Human No 6.3 EC50 = 563 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4cccc(Cl)c4[nH]3)CC2)cc1
CHEMBL3287395 drd3_human Human No 7.2 EC50 = 57 nM Funct
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
490 9 0 7 4.8 CCOC(=O)C1=NN2C=CC(=CC2=C1)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3800194 drd3_human Human No 7.2 EC50 = 57.8 nM Funct
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
457 6 1 4 5.2 O=C(NCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1cccc2ccccc12
CHEMBL4455487 drd3_human Human No 6.2 EC50 = 576 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4cnccc4[nH]3)CC2)cc1
CHEMBL4591958 drd3_human Human No 7.2 EC50 = 59 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc2[nH]c(C(=O)N3CCN(CCOc4cccnc4)CC3)cc2c1
CHEMBL4471669 drd3_human Human No 6.2 EC50 = 590 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1
CHEMBL3590082 drd3_human Human No 8.2 EC50 = 6.1 nM Funct
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
414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1
CHEMBL59 drd3_human Human Yes 8.2 EC50 = 6.1 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4091498 drd3_human Human No 8.2 EC50 = 6.1 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL4091498 drd3_human Human No 8.2 EC50 = 6.2 nM Funct
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
526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1
CHEMBL3799603 drd3_human Human No 8.2 EC50 = 6.3 nM Funct
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
421 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccccc1
CHEMBL69451 drd3_human Human Yes 8.2 EC50 = 6.3 nM Funct
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
482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL69451 drd3_human Human Yes 8.2 EC50 = 6.3 nM Funct
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
482 8 1 4 5.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL59 drd3_human Human Yes 8.2 EC50 = 6.4 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4458958 drd3_human Human No 8.2 EC50 = 6.4 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc2cc(C(=O)N3CCN(CCOc4cccnc4)CC3)[nH]c2c1
CHEMBL4071240 drd3_human Human No 8.2 EC50 = 6.5 nM Funct
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
540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1
CHEMBL3798504 drd3_human Human No 8.2 EC50 = 6.6 nM Funct
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
515 8 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(C(=O)O)c2ccccc12
CHEMBL3800681 drd3_human Human No 8.2 EC50 = 6.6 nM Funct
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
515 8 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(C(=O)O)c2ccccc12
CHEMBL3798211 drd3_human Human No 8.2 EC50 = 6.8 nM Funct
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
514 8 2 5 4.9 NC(=O)c1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12
CHEMBL3800682 drd3_human Human No 8.2 EC50 = 6.8 nM Funct
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
514 8 2 5 4.9 NC(=O)c1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12
CHEMBL4575155 drd3_human Human No 8.2 EC50 = 6.9 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 1 4 2.7 Cc1cccc2[nH]c(C(=O)N3CCN(CCOc4cccnc4)CC3)cc12
CHEMBL3800421 drd3_human Human No 8.2 EC50 = 6.9 nM Funct
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
460 7 2 4 5.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]ccc12
CHEMBL4086944 drd3_human Human No 8.2 EC50 = 6.9 nM Funct
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
556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL168357 drd3_human Human No 7.2 EC50 = 60.3 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2ccccc12
CHEMBL4550539 drd3_human Human No 7.2 EC50 = 60.9 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
388 5 2 3 3.5 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc3[nH]ccc3c2)CC1
CHEMBL4519087 drd3_human Human No 6.2 EC50 = 610 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
377 5 1 3 3.6 Cc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1C
CHEMBL4514648 drd3_human Human No 6.2 EC50 = 611 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4cc(C)ccc4[nH]3)CC2)cc1
CHEMBL4091064 drd3_human Human No 7.2 EC50 = 62 nM Funct
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
456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12
CHEMBL4437215 drd3_human Human No 7.2 EC50 = 63 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1cc2cnccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4446145 drd3_human Human No 6.2 EC50 = 630 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
395 6 1 4 3.7 CSc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL168948 drd3_human Human No 6.2 EC50 = 631.0 nM Funct
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
487 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)[C@H]1CC[C@@H](c2ccccc2)CC1
CHEMBL4448320 drd3_human Human Yes 5.2 EC50 = 6354 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1
CHEMBL4063282 drd3_human Human No 7.2 EC50 = 66 nM Funct
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
393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1
CHEMBL3287390 drd3_human Human No 7.2 EC50 = 66 nM Funct
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
418 7 0 5 4.6 C1CN(CCN1CCCCOC2=CC3=CC=NN3C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287390 drd3_human Human No 7.2 EC50 = 66.1 nM Funct
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
418 7 0 5 4.6 C1CN(CCN1CCCCOC2=CC3=CC=NN3C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL246855 drd3_human Human Yes 6.2 EC50 = 661 nM Funct
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
424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21
CHEMBL4082631 drd3_human Human No 6.2 EC50 = 667 nM Funct
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
312 3 0 1 6.4 CCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21
CHEMBL419792 drd3_human Human Yes 6.2 EC50 = 669 nM Bind
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3
CHEMBL4099236 drd3_human Human No 7.2 EC50 = 67.6 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL4116199 drd3_human Human No 7.2 EC50 = 67.6 nM Funct
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
502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL3590081 drd3_human Human No 7.2 EC50 = 68 nM Funct
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
396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1
CHEMBL30208 drd3_human Human No 7.2 EC50 = 68 nM Funct
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
467 6 1 4 4.2 COc1c(C(=O)NCCN2CCN(c3ccccc3)CC2)cc(Br)c2ccccc12
CHEMBL29182 drd3_human Human No 7.2 EC50 = 68 nM Funct
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
495 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(C)c3C)CC2)cc(Br)c2ccccc12
CHEMBL4105030 drd3_human Human No 7.2 EC50 = 69.2 nM Funct
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
423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1
CHEMBL4538010 drd3_human Human No 8.2 EC50 = 7 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
350 5 1 4 2.4 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL53 drd3_human Human Yes 8.2 EC50 = 7 nM Funct
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 7.3 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL3799902 drd3_human Human No 8.1 EC50 = 7.4 nM Funct
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
457 6 1 4 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2ccccc12
CHEMBL4072282 drd3_human Human No 8.1 EC50 = 7.4 nM Funct
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
488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1
CHEMBL3798331 drd3_human Human No 8.1 EC50 = 7.5 nM Funct
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
461 7 2 5 4.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]cnc12
CHEMBL3800685 drd3_human Human No 8.1 EC50 = 7.5 nM Funct
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
461 7 2 5 4.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2[nH]cnc12
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 7.6 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4098236 drd3_human Human No 8.1 EC50 = 7.7 nM Funct
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
408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1
CHEMBL162762 drd3_human Human Yes 8.1 EC50 = 7.7 nM Funct
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
205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1
CHEMBL4098236 drd3_human Human No 8.1 EC50 = 7.8 nM Funct
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
408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1
CHEMBL4105030 drd3_human Human No 7.2 EC50 = 70 nM Funct
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
423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1
CHEMBL4103339 drd3_human Human No 7.2 EC50 = 70 nM Funct
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
483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL4103339 drd3_human Human No 7.2 EC50 = 70.8 nM Funct
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
483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1
CHEMBL1700053 drd3_human Human Yes 6.2 EC50 = 710 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
370 7 0 5 2.5 COc1ccc(OCCN2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1
CHEMBL4473158 drd3_human Human No 6.2 EC50 = 710 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1OC
CHEMBL4469777 drd3_human Human No 6.2 EC50 = 710 nM Bind
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl
CHEMBL3800575 drd3_human Human No 7.1 EC50 = 76.5 nM Funct
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
475 7 1 4 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1CCCC2
CHEMBL3590082 drd3_human Human No 7.1 EC50 = 79 nM Funct
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
414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1
CHEMBL4088639 drd3_human Human No 7.1 EC50 = 79 nM Funct
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
421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1
CHEMBL250403 drd3_human Human Yes 8.1 EC50 = 8 nM Funct
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
221 3 1 3 2.2 CCCN1CCO[C@H](c2cccc(O)c2)C1
CHEMBL240773 drd3_human Human Yes 8.1 EC50 = 8.4 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 8.5 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 8.5 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 8.5 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 8.5 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.1 EC50 = 8.6 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4468192 drd3_human Human No 7.1 EC50 = 80 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 1 4 2.7 Cc1c(C(=O)N2CCN(CCOc3cccnc3)CC2)[nH]c2ccccc12
CHEMBL240773 drd3_rat Rat Yes 7.1 EC50 = 80 nM Bind
Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligandBasal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL4556267 drd3_human Human No 7.1 EC50 = 81 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
351 5 1 5 1.8 O=C(c1cc2ccncc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4575347 drd3_human Human No 6.1 EC50 = 810 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4ccncc4[nH]3)CC2)cc1
CHEMBL4585649 drd3_human Human No 7.1 EC50 = 82 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
393 6 1 4 3.4 COc1ccc(OC(C)CN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL59 drd3_human Human Yes 6.1 EC50 = 820 nM Bind
Agonist activity at RLuc8-fused human D3R Y198A/Y365A double mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y198A/Y365A double mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL30206 drd3_human Human No 7.1 EC50 = 83 nM Funct
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)cc(Br)c2ccccc12
CHEMBL1627318 drd3_human Human No 7.1 EC50 = 84 nM Funct
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
587 7 2 5 4.6 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1
CHEMBL4476784 drd3_human Human Yes 7.1 EC50 = 86 nM Funct
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
379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1
CHEMBL401328 drd3_human Human Yes 6.1 EC50 = 864 nM Funct
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
179 1 2 3 1.1 Oc1cccc(C2CNCCO2)c1
CHEMBL4439544 drd3_human Human Yes 7.1 EC50 = 87 nM Funct
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
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL4596514 drd3_human Human Yes 7.1 EC50 = 87 nM Funct
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
471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl
CHEMBL370297 drd3_human Human No 8.0 EC50 = 9.1 nM Funct
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
None None None None
CHEMBL4086944 drd3_human Human No 8.0 EC50 = 9.1 nM Funct
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
556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL4574338 drd3_human Human Yes 8.0 EC50 = 9.2 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
349 5 1 3 3.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccccc2)CC1
CHEMBL4086944 drd3_human Human No 8.0 EC50 = 9.2 nM Funct
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
556 8 2 5 5.4 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1
CHEMBL2203406 drd3_human Human No 8.0 EC50 = 9.3 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1
CHEMBL59 drd3_human Human Yes 8.0 EC50 = 9.3 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL59 drd3_human Human Yes 8.0 EC50 = 9.3 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4435730 drd3_human Human No 8.0 EC50 = 9.5 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
364 5 0 5 2.4 Cn1cc(C(=O)N2CCN(CCOc3cccnc3)CC2)c2ccccc21
CHEMBL4087187 drd3_human Human No 8.0 EC50 = 9.6 nM Funct
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
408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1
CHEMBL4087187 drd3_human Human No 8.0 EC50 = 9.7 nM Funct
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
408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1
CHEMBL240773 drd3_human Human Yes 8.0 EC50 = 9.7 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL240773 drd3_human Human Yes 8.0 EC50 = 9.8 nM Funct
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
219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2
CHEMBL195083 drd3_human Human No 8.0 EC50 = 9.8 nM Funct
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
None None None None
CHEMBL7549 drd3_human Human Yes 8.0 EC50 = 9.8 nM Funct
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1
CHEMBL445102 drd3_human Human Yes 7.0 EC50 = 90.4 nM Funct
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
340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2
CHEMBL4090459 drd3_human Human No 7.0 EC50 = 93 nM Funct
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
489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1
CHEMBL4090459 drd3_human Human No 7.0 EC50 = 93.3 nM Funct
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
489 10 1 6 5.1 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1ccccc1
CHEMBL4564115 drd3_human Human No 5.0 EC50 = 9300 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 7 0 5 2.9 COc1ccc(OCC(C)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1
CHEMBL3798179 drd3_human Human No 7.0 EC50 = 94.3 nM Bind
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
417 7 3 4 2.9 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)[C@@H]3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL4464861 drd3_human Human No 6.0 EC50 = 970 nM Bind
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1
CHEMBL4553903 drd3_human Human Yes 5.0 EC50 = 9700 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
278 5 0 4 1.2 COc1ccc(OCCN2CCN(C(C)=O)CC2)cc1
CHEMBL4466214 drd3_human Human No 7.0 EC50 = 98 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
384 5 1 4 3.1 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCN(CCOc2cccnc2)CC1
CHEMBL4552311 drd3_human Human No 7.0 EC50 = 98 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
370 7 0 5 2.5 COc1ccc(C(=O)N2CCN(CCOc3cccc(OC)c3)CC2)cc1
CHEMBL400827 drd3_human Human Yes 7.0 EC50 = 98.6 nM Funct
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
354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21
CHEMBL4548345 drd3_human Human No 6.0 EC50 = 980 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4cccc(OC)c4[nH]3)CC2)cc1
CHEMBL4580817 drd3_human Human Yes 7.0 EC50 = 99.2 nM Funct
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
482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4597188 drd3_human Human Yes 7.0 EC50 = 99.2 nM Funct
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
482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl
CHEMBL4443381 drd3_human Human No 6.0 EC50 = 997 nM Bind
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
397 5 1 3 4.0 Cc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1Cl
CHEMBL54 drd3_human Human Yes 10.2 IC50 = 0.1 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL157138 drd3_human Human Yes 9.8 IC50 = 0.2 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL3322994 drd3_human Human No 9.7 IC50 = 0.2 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
445 7 1 5 4.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn2ccccc2n1
CHEMBL240693 drd3_rat Rat No 9.7 IC50 = 0.2 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
496 7 1 5 4.4 O=S(=O)(N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1)c1cccnc1
CHEMBL424294 drd3_human Human Yes 9.7 IC50 = 0.2 nM Funct
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
423 8 1 5 4.2 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4S3
CHEMBL54 drd3_human Human Yes 9.6 IC50 = 0.3 nM Funct
Antagonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta arrestin2 recruitment preincubated for 30 mins followed by dopamine addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta arrestin2 recruitment preincubated for 30 mins followed by dopamine addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL2024516 drd3_rat Rat No 9.6 IC50 = 0.3 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
411 6 1 3 4.6 CCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
CHEMBL2024514 drd3_rat Rat No 9.5 IC50 = 0.3 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
397 5 1 3 4.2 CC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
CHEMBL3323016 drd3_human Human No 9.5 IC50 = 0.3 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
504 7 1 8 3.2 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccncc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL3323017 drd3_human Human No 9.5 IC50 = 0.3 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
538 7 1 8 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4nc(Cl)ccc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL391700 drd3_rat Rat No 9.5 IC50 = 0.3 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
496 7 1 5 4.2 O=S(=O)(N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1)c1cccnc1
CHEMBL2024520 drd3_rat Rat No 9.5 IC50 = 0.3 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
398 5 2 3 3.7 NC(=O)N[C@H]1CC[C@H](CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1
CHEMBL3323016 drd3_human Human No 9.5 IC50 = 0.3 nM Funct
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
504 7 1 8 3.2 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccncc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL2024518 drd3_rat Rat No 9.5 IC50 = 0.3 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
426 6 2 3 4.4 CCNC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
CHEMBL267930 drd3_human Human Yes 9.4 IC50 = 0.4 nM Bind
Displacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrs
395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL3323015 drd3_human Human No 9.4 IC50 = 0.4 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
504 7 1 8 3.2 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4cccnc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL428910 drd3_rat Rat No 9.4 IC50 = 0.4 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
521 7 1 6 4.0 N#Cc1cc(N2CCN(CC[C@H]3CC[C@H](NS(=O)(=O)c4cccnc4)CC3)CC2)cc(C(F)(F)F)c1
CHEMBL25236 drd3_rat Rat Yes 9.4 IC50 = 0.4 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL2024513 drd3_rat Rat No 9.4 IC50 = 0.4 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
451 5 1 3 4.7 O=C(N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1)C(F)(F)F
CHEMBL2024515 drd3_rat Rat No 9.3 IC50 = 0.5 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
433 6 1 4 3.6 CS(=O)(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
CHEMBL239847 drd3_rat Rat No 9.3 IC50 = 0.5 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
565 9 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](CCN3CCN(c4ccc(Br)cc4OC)CC3)CC2)cc1
CHEMBL240271 drd3_rat Rat No 9.3 IC50 = 0.5 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
574 9 1 5 6.1 O=S(=O)(N[C@H]1CC[C@H](CCN2CCC(Cc3cccc(C(F)(F)F)c3)CC2)CC1)c1ccc(-n2cccn2)cc1
CHEMBL315772 drd3_human Human No 9.3 IC50 = 0.5 nM Bind
Binding affinity against Dopamine receptor D3Binding affinity against Dopamine receptor D3
328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1
CHEMBL315772 drd3_human Human No 9.3 IC50 = 0.5 nM Bind
Binding affinity for human cloned Dopamine receptor D3Binding affinity for human cloned Dopamine receptor D3
328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1
CHEMBL1403281 drd3_human Human Yes 9.2 IC50 = 0.6 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
575 5 3 6 2.4 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)C(C)C)O)C
CHEMBL726 drd3_human Human Yes 9.2 IC50 = 0.6 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F
CHEMBL493 drd3_human Human Yes 9.2 IC50 = 0.6 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
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
CHEMBL3323011 drd3_human Human No 9.2 IC50 = 0.6 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL2024519 drd3_rat Rat No 9.2 IC50 = 0.6 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
454 7 1 3 5.1 CCN(CC)C(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
CHEMBL3322993 drd3_human Human No 9.2 IC50 = 0.7 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cn3ccccc3n2)CC1
CHEMBL240273 drd3_rat Rat No 9.2 IC50 = 0.7 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
589 7 2 6 4.5 N#Cc1cc(N2CCN(CC[C@H]3CC[C@H](NS(=O)(=O)c4ccc5c(c4)CCC(=O)N5)CC3)CC2)cc(C(F)(F)F)c1
CHEMBL429093 drd3_rat Rat No 9.2 IC50 = 0.7 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
512 9 1 7 3.6 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](CCN3CCN(c4cccc(C#N)c4)CC3)CC2)cc1OC
CHEMBL25236 drd3_rat Rat Yes 9.1 IC50 = 0.7 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL3084515 drd3_human Human No 9.1 IC50 = 0.9 nM Funct
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12
CHEMBL392528 drd3_rat Rat No 9.1 IC50 = 0.9 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
577 8 2 6 4.6 CC(=O)Nc1ccc(S(=O)(=O)N[C@H]2CC[C@H](CCN3CCN(c4cc(C#N)cc(C(F)(F)F)c4)CC3)CC2)cc1
CHEMBL2024509 drd3_rat Rat No 9.1 IC50 = 0.9 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
458 6 1 5 3.2 CS(=O)(=O)N[C@H]1CC[C@H](CCN2CCN(c3cc(C#N)cc(C(F)(F)F)c3)CC2)CC1
CHEMBL244562 drd3_human Human No 9.0 IC50 = 1 nM Funct
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
496 7 2 4 4.5 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc(=O)[nH]2)cc1
CHEMBL244562 drd3_human Human No 9.0 IC50 = 1 nM Bind
Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.
496 7 2 4 4.5 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc(=O)[nH]2)cc1
CHEMBL244990 drd3_human Human No 9.0 IC50 = 1 nM Bind
Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.
498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL240480 drd3_rat Rat No 9.0 IC50 = 1 nM Bind
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat dopamine D3 receptor expressed in Sf9 cells
581 8 2 6 4.8 O=C1COc2ccc(S(=O)(=O)N[C@H]3CC[C@H](CCN4CCC(Oc5cccc(C(F)(F)F)c5)CC4)CC3)cc2N1
CHEMBL195057 drd3_human Human No 9.0 IC50 = 1 nM Funct
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
419 6 2 4 3.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(O)cc1
CHEMBL1627304 drd3_human Human No 9.0 IC50 = 1.1 nM Funct
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
421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1
CHEMBL285755 drd3_rat Rat Yes 9.0 IC50 = 1.1 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC
CHEMBL416047 drd3_rat Rat No 9.0 IC50 = 1.1 nM Bind
Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatumConcentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum
399 5 2 6 1.3 CCN1CCN(C)C[C@@H](NC(=O)c2cc(Br)c(NC)nc2OC)C1
CHEMBL244774 drd3_human Human No 8.9 IC50 = 1.2 nM Funct
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
496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1
CHEMBL244774 drd3_human Human No 8.9 IC50 = 1.2 nM Bind
Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.
496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1
CHEMBL1255588 drd3_human Human Yes 8.9 IC50 = 1.2 nM Bind
Binding affinity to human dopamine D3 receptor by radioligand displacement assayBinding affinity to human dopamine D3 receptor by radioligand displacement assay
361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1
CHEMBL285755 drd3_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC
CHEMBL3323011 drd3_human Human No 8.9 IC50 = 1.3 nM Funct
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
503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL194837 drd3_human Human No 8.9 IC50 = 1.3 nM Bind
Inhibitory concentration against dopamine receptor D3Inhibitory concentration against dopamine receptor D3
447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12
CHEMBL3946995 drd3_human Human No 8.9 IC50 = 1.4 nM Funct
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
438 6 1 6 4.4 O=C(N[C@H]1CC[C@H](CCN2CCN(c3nsc4ccccc34)CC2)CC1)c1ccco1
CHEMBL1627314 drd3_human Human No 8.8 IC50 = 1.5 nM Funct
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
490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1
CHEMBL1627315 drd3_human Human No 8.8 IC50 = 1.6 nM Funct
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
452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1
CHEMBL3885419 drd3_human Human No 8.8 IC50 = 1.6 nM Bind
Displacement of [3H]methyl-spiperone from human recombinant dopamine D3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]methyl-spiperone from human recombinant dopamine D3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
361 0 1 2 4.8 CC(C)(C)[C@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1
CHEMBL8514 drd3_human Human Yes 8.8 IC50 = 1.6 nM Bind
Displacement of [3H]methylspiperone from human recombinant Dopamine D3 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D3 receptor expressed in CHO cells
361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C
CHEMBL2028019 drd3_rat Rat No 8.8 IC50 = 1.6 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL1627311 drd3_human Human No 8.8 IC50 = 1.8 nM Funct
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
440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1
CHEMBL3322995 drd3_human Human No 8.7 IC50 = 1.8 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
445 7 1 5 3.7 O=C(NCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1cn2ccccc2n1
CHEMBL25236 drd3_human Human Yes 8.7 IC50 = 1.8 nM Funct
Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL1255588 drd3_human Human Yes 8.7 IC50 = 1.9 nM Bind
Binding affinity to human dopamine D3 receptor by radioligand displacement assayBinding affinity to human dopamine D3 receptor by radioligand displacement assay
361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1
CHEMBL2024506 drd3_rat Rat No 8.7 IC50 = 1.9 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
397 5 1 3 3.9 CC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1
CHEMBL2024508 drd3_rat Rat No 8.7 IC50 = 1.9 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
422 5 1 4 3.8 CC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cc(C#N)cc(C(F)(F)F)c3)CC2)CC1
CHEMBL54 drd3_human Human Yes 8.0 IC50 = 10 nM Bind
Binding affinity towards human Dopamine receptor D3Binding affinity towards human Dopamine receptor D3
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL1255588 drd3_human Human Yes 8.0 IC50 = 10 nM Bind
Inhibition of human dopamine D3 receptorInhibition of human dopamine D3 receptor
361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1
CHEMBL3084503 drd3_human Human No 8.0 IC50 = 10.2 nM Funct
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12
CHEMBL4570554 drd3_human Human No 6.0 IC50 = 1020 nM Bind
Antagonist activity at human D3 receptor expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesisAntagonist activity at human D3 receptor expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis
484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1
CHEMBL589 drd3_rat Rat Yes 7.0 IC50 = 107 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O
CHEMBL83 drd3_human Human Yes 6.0 IC50 = 1072 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1
CHEMBL1086756 drd3_human Human No 6.0 IC50 = 1072 nM Bind
Inhibition of dopamine D3 receptorInhibition of dopamine D3 receptor
512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C
CHEMBL964 drd3_human Human Yes 6.0 IC50 = 1084 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL2024511 drd3_rat Rat No 8.0 IC50 = 11 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
447 7 1 4 3.3 CS(=O)(=O)N[C@H]1CC[C@H](CCN2CCN(Cc3cccc(C(F)(F)F)c3)CC2)CC1
CHEMBL1627317 drd3_human Human No 8.0 IC50 = 11.2 nM Funct
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
423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1
CHEMBL64671 drd3_human Human No 6.0 IC50 = 1100 nM Bind
Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.
360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1
CHEMBL59 drd3_rat Rat Yes 7.0 IC50 = 111 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL69571 drd3_human Human No 6.9 IC50 = 114 nM Funct
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
491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2
CHEMBL1774540 drd3_human Human No 5.9 IC50 = 1140 nM Funct
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
454 9 2 5 3.5 COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1
CHEMBL84158 drd3_human Human Yes 5.9 IC50 = 1149 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC
CHEMBL716 drd3_human Human Yes 5.9 IC50 = 1163.2 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2
CHEMBL1222364 drd3_human Human No 5.9 IC50 = 1171 nM Bind
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cellsDisplacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cells
409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL1222234 drd3_human Human No 5.9 IC50 = 1195 nM Bind
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cellsDisplacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cells
423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12
CHEMBL71 drd3_human Human Yes 7.9 IC50 = 12 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C
CHEMBL1627308 drd3_human Human No 7.9 IC50 = 12.1 nM Funct
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
422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1
CHEMBL3084502 drd3_human Human No 7.9 IC50 = 12.3 nM Funct
Antagonist activity at dopamine D3 receptorAntagonist activity at dopamine D3 receptor
366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12
CHEMBL242644 drd3_human Human No 7.9 IC50 = 12.8 nM Funct
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
460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1
CHEMBL242644 drd3_human Human No 7.9 IC50 = 12.8 nM Bind
Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.
460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1
CHEMBL3322998 drd3_human Human No 6.9 IC50 = 120 nM Bind
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs by [3H]thymidine uptake assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs by [3H]thymidine uptake assay
428 7 1 6 3.2 O=C(NCCCCN1CCN(c2ccnc3ccccc23)CC1)c1cn2ccccc2n1
CHEMBL415300 drd3_human Human Yes 6.9 IC50 = 120 nM Bind
Binding affinity towards human Dopamine receptor D3Binding affinity towards human Dopamine receptor D3
326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1
CHEMBL8412 drd3_human Human Yes 5.9 IC50 = 1200 nM Bind
Inhibition of dopamine D3 receptorInhibition of dopamine D3 receptor
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL633 drd3_human Human Yes 5.9 IC50 = 1208 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL305660 drd3_human Human Yes 6.9 IC50 = 121.6 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL1123 drd3_human Human Yes 5.9 IC50 = 1210 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC
CHEMBL1774535 drd3_human Human No 5.9 IC50 = 1220 nM Funct
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
462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1
CHEMBL267044 drd3_human Human Yes 6.9 IC50 = 123 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
341 6 2 5 0.6 CCN1CCC[C@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N
CHEMBL59 drd3_rat Rat Yes 6.9 IC50 = 124 nM Bind
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation countingDisplacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL1774532 drd3_human Human No 5.9 IC50 = 1240 nM Funct
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
455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1
CHEMBL25236 drd3_human Human Yes 7.9 IC50 = 13 nM Bind
Antagonist activity at human dopamine D3 receptor expressed in human U2OS cells assessed as inhibition of pramipexole-stimulated beta-arrestin recruitmentAntagonist activity at human dopamine D3 receptor expressed in human U2OS cells assessed as inhibition of pramipexole-stimulated beta-arrestin recruitment
417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2
CHEMBL728 drd3_human Human Yes 7.9 IC50 = 13 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL3696485 drd3_rat Rat No 7.9 IC50 = 13.2 nM Bind
Receptor Assay: Competitive binding test for receptors: 20 μl of each of the test compounds and 20 μl of the radioactive ligand together with 160 μl of the receptor proteins were added into the reaction tubes, and the final concentrations of the test compound and the positive drug were all 10 μmol/L. After 50 min of incubation in 30° C. water bath, the tubes were immediately moved to ice bath to terminate the reactions. GF/C glass fiber filter papers were used for rapid sucking filtration on a Millipore cell sample collector, elution buffer (50 mM Tris-HCl, PH 7.4) was applied for 3 ml×3 times, and microwave was applied for 4-5 min for drying. The filter papers were moved into 0.5 ml centrifuge tubes, and 500 μl of lipid-soluble scintillation solution was added. The tubes were allowed to stand still for over 30 min in dark, and the intensities of radioactivity were measured by a counter.Receptor Assay: Competitive binding test for receptors: 20 μl of each of the test compounds and 20 μl of the radioactive ligand together with 160 μl of the receptor proteins were added into the reaction tubes, and the final concentrations of the test compound and the positive drug were all 10 μmol/L. After 50 min of incubation in 30° C. water bath, the tubes were immediately moved to ice bath to terminate the reactions. GF/C glass fiber filter papers were used for rapid sucking filtration on a Millipore cell sample collector, elution buffer (50 mM Tris-HCl, PH 7.4) was applied for 3 ml×3 times, and microwave was applied for 4-5 min for drying. The filter papers were moved into 0.5 ml centrifuge tubes, and 500 μl of lipid-soluble scintillation solution was added. The tubes were allowed to stand still for over 30 min in dark, and the intensities of radioactivity were measured by a counter.
462 8 1 6 4.1 O=c1oc2cc(OCCCCN3CCN(c4ccccc4CO)CC3)ccc2c2c1CCCC2
CHEMBL1627316 drd3_human Human No 7.9 IC50 = 13.7 nM Funct
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
461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1
CHEMBL1642116 drd3_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D3 receptor expressed in cells
435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1
CHEMBL546257 drd3_human Human Yes 5.9 IC50 = 1318 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL554190 drd3_human Human Yes 5.9 IC50 = 1318 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL7568 drd3_human Human Yes 5.9 IC50 = 1318 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL954 drd3_human Human Yes 5.9 IC50 = 1319 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1
CHEMBL841 drd3_human Human Yes 5.9 IC50 = 1337 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1
CHEMBL1113 drd3_human Human Yes 6.9 IC50 = 134 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1
CHEMBL1200710 drd3_human Human Yes 6.9 IC50 = 139 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL415 drd3_human Human Yes 6.9 IC50 = 139 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL1628227 drd3_human Human Yes 5.9 IC50 = 1393 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21
CHEMBL3323019 drd3_human Human No 7.9 IC50 = 14 nM Bind
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assayAntagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
559 9 2 6 4.7 CN(C)Cc1c(C(=O)NCCCCN2CCN(c3cc(C(F)(F)F)nc(C(C)(C)C)n3)CC2)[nH]c2ccccc12
CHEMBL84931 drd3_human Human No 7.9 IC50 = 14.1 nM Bind
Binding affinity for human cloned Dopamine receptor D3Binding affinity for human cloned Dopamine receptor D3
312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1
CHEMBL231156 drd3_human Human No 7.8 IC50 = 14.3 nM Funct
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
494 7 1 4 5.2 O=C(NC[C@H]1C[C@@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1
CHEMBL40497 drd3_rat Rat No 7.8 IC50 = 14.3 nM Bind
Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatumConcentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum
399 5 2 6 1.3 CCN1CCN(C)C[C@H](NC(=O)c2cc(Br)c(NC)nc2OC)C1
CHEMBL300780 drd3_human Human Yes 7.8 IC50 = 14.4 nM Funct
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
493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL300780 drd3_human Human Yes 7.8 IC50 = 14.4 nM Funct
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
493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL1627319 drd3_human Human No 7.8 IC50 = 14.5 nM Funct
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
549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1
CHEMBL458397 drd3_rat Rat No 7.8 IC50 = 14.7 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cells
343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL465054 drd3_rat Rat No 7.8 IC50 = 14.7 nM Bind
Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cellsDisplacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cells
343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL1627324 drd3_human Human No 7.8 IC50 = 14.9 nM Funct
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
405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1
CHEMBL1221449 drd3_human Human No 5.9 IC50 = 1426 nM Bind
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cellsDisplacement of [3H]spiperone from human dopamine D3 receptor expressed in CHOKI cells
435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1
CHEMBL496739 drd3_human Human Yes 6.8 IC50 = 143 nM Funct
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
391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1
CHEMBL1774533 drd3_human Human No 5.8 IC50 = 1430 nM Funct
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
493 8 1 5 5.0 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1
CHEMBL1729 drd3_human Human Yes 6.8 IC50 = 144 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 drd3_human Human Yes 6.8 IC50 = 144 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL115280 drd3_human Human No 6.8 IC50 = 149 nM Bind
Inhibition of human dopamine receptor D3Inhibition of human dopamine receptor D3
413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2
CHEMBL40082 drd3_rat Rat No 7.8 IC50 = 15.1 nM Bind
Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum.Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum.
354 5 2 5 1.8 CCN1CCN(C)C[C@@H](NC(=O)c2cc(Cl)c(NC)cc2OC)C1
CHEMBL3696484 drd3_rat Rat No 7.8 IC50 = 15.1 nM Bind
Receptor Assay: Competitive binding test for receptors: 20 μl of each of the test compounds and 20 μl of the radioactive ligand together with 160 μl of the receptor proteins were added into the reaction tubes, and the final concentrations of the test compound and the positive drug were all 10 μmol/L. After 50 min of incubation in 30° C. water bath, the tubes were immediately moved to ice bath to terminate the reactions. GF/C glass fiber filter papers were used for rapid sucking filtration on a Millipore cell sample collector, elution buffer (50 mM Tris-HCl, PH 7.4) was applied for 3 ml×3 times, and microwave was applied for 4-5 min for drying. The filter papers were moved into 0.5 ml centrifuge tubes, and 500 μl of lipid-soluble scintillation solution was added. The tubes were allowed to stand still for over 30 min in dark, and the intensities of radioactivity were measured by a counter.Receptor Assay: Competitive binding test for receptors: 20 μl of each of the test compounds and 20 μl of the radioactive ligand together with 160 μl of the receptor proteins were added into the reaction tubes, and the final concentrations of the test compound and the positive drug were all 10 μmol/L. After 50 min of incubation in 30° C. water bath, the tubes were immediately moved to ice bath to terminate the reactions. GF/C glass fiber filter papers were used for rapid sucking filtration on a Millipore cell sample collector, elution buffer (50 mM Tris-HCl, PH 7.4) was applied for 3 ml×3 times, and microwave was applied for 4-5 min for drying. The filter papers were moved into 0.5 ml centrifuge tubes, and 500 μl of lipid-soluble scintillation solution was added. The tubes were allowed to stand still for over 30 min in dark, and the intensities of radioactivity were measured by a counter.
509 7 0 7 5.5 O=c1oc2c(Cl)c(OCCCCN3CCN(c4nsc5ccccc45)CC3)ccc2c2c1CCC2
CHEMBL302183 drd3_human Human No 6.8 IC50 = 150 nM Bind
Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.
349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1
CHEMBL17157 drd3_human Human Yes 5.8 IC50 = 1503 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O
CHEMBL1642118 drd3_human Human No 5.8 IC50 = 1520 nM Bind
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D3 receptor expressed in cells
449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1
CHEMBL114 drd3_human Human Yes 4.8 IC50 = 15366 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1
CHEMBL114484 drd3_human Human No 6.8 IC50 = 154 nM Bind
Inhibition of human dopamine receptor D3Inhibition of human dopamine receptor D3
355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1
CHEMBL565552 drd3_human Human No 5.8 IC50 = 1558 nM Bind
Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO-K1 cellsDisplacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO-K1 cells
379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21
CHEMBL81 drd3_human Human Yes 5.8 IC50 = 1565 nM Bind
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O
CHEMBL3323011 drd3_human Human No 6.8 IC50 = 157 nM Bind
Antagonist activity against human D3R expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs by [3H]thymidine uptake assayAntagonist activity against human D3R expressed in CHO cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs by [3H]thymidine uptake assay
503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)cc(C(F)(F)F)n1
CHEMBL8514</