ChEMBL ligand: CHEMBL85606 (SB-277011)
D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] There should be some charts here, you may need to enable JavaScript!
D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] There should be some charts here, you may need to enable JavaScript!
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis	B	5.29	pKi	5160	nM	Ki	J Med Chem (2017) 60: 1478-1494 [PMID:28186762]
ChEMBL	Inhibition of [125I]iodosulpiride binding to human Dopamine D2L receptor expressed in CHO cells	B	5.98	pKi	1050	nM	Ki	J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
ChEMBL	Displacement of [125I]iodosulpiride from human Dopamine receptor D2 expressed in CHO cells	B	6	pKi	1000	nM	Ki	Bioorg Med Chem Lett (2001) 11: 685-688 [PMID:11266169]
ChEMBL	Binding affinity towards human Dopamine receptor D2 by displacement of [125I]iodosulpiride expressed in CHO cells	B	6	pKi	1000	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2553-2555 [PMID:11086728]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2 receptor expressed in CHO-K1 cell membranes after 120 mins by liquid scintillation counter method	B	6.3	pKi	501.19	nM	Ki	Bioorg Med Chem (2016) 24: 1619-1636 [PMID:26951894]
ChEMBL	Displacement of [125I]-7-OH-PIPAT from rat brain dopamine D2 receptor after 45 mins by microplate scintillation counting analysis	B	6.3	pKi	501.19	nM	Ki	Bioorg Med Chem Lett (2016) 26: 1329-1332 [PMID:26786693]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2 receptor expressed in CHO-K1 cell membranes coexpressing Galpha16 after 120 mins by liquid scintillation counting	B	6.31	pKi	489.78	nM	Ki	J Med Chem (2016) 59: 8549-8576 [PMID:27564135]
ChEMBL	Binding affinity to human DRD2 receptor by GTPgammaS binding assay	B	6.4	pKi	398.11	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5056-5059 [PMID:19635669]
ChEMBL	Antagonist activity at human Dopamine D2 receptor expressed in CHO cell by GTPgammaS binding assay	F	6.4	pKi	398.11	nM	Ki	J Med Chem (2010) 53: 374-391 [PMID:19891474]
ChEMBL	Antagonist activity at dopamine D2 receptor by GTPgammaS binding assay	F	6.4	pKi	398.11	nM	Ki	Bioorg Med Chem Lett (2008) 18: 908-912 [PMID:18178090]
ChEMBL	Displacement of [35S]GTP-gamma-S from human cloned dopamine D2 receptor expressed in CHO cells after 30 mins	F	6.4	pKi	398.11	nM	Ki	J Med Chem (2007) 50: 5076-5089 [PMID:17867665]
ChEMBL	Antagonist activity at dopamine D2 receptor by GTPgammaS binding assay	F	6.4	pKi	398.11	nM	Ki	Bioorg Med Chem Lett (2008) 18: 901-907 [PMID:18248991]
ChEMBL	Antagonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay	F	6.4	pKi	398.11	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4799-4801 [PMID:19560918]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Inhibition of [125I]iodosulpiride binding to rat Dopamine D2 receptor expressed in CHO cells	B	5.55	pKi	2820	nM	Ki	J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Agonist activity at human dopamine D3 receptor expressed in CHO cells after 90 mins by [35S]-GTPgamma S assay	B	5	pKi	>10000	nM	Ki	Bioorg Med Chem Lett (2016) 26: 1329-1332 [PMID:26786693]
ChEMBL	Inhibition of [125I]iodosulpiride binding to human Dopamine D3 receptor expressed in CHO cells	B	7.95	pKi	11.2	nM	Ki	J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis	B	7.96	pKi	11	nM	Ki	J Med Chem (2017) 60: 1478-1494 [PMID:28186762]
GtoPdb	-	-	8	pKi	10	nM	Ki	J Pharmacol Exp Ther (2000) 294: 1154-65 [PMID:10945872]
ChEMBL	Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (2001) 11: 685-688 [PMID:11266169]
ChEMBL	Binding affinity towards human Dopamine receptor D3 by displacement of [125I]iodosulpiride expressed in CHO cells	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2553-2555 [PMID:11086728]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D3 receptor expressed in CHO-K1 cell membranes after 90 mins by liquid scintillation counting	B	8.19	pKi	6.46	nM	Ki	J Med Chem (2016) 59: 8549-8576 [PMID:27564135]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D3 receptor expressed in CHO-K1 cell membranes after 90 mins by liquid scintillation counter method	B	8.2	pKi	6.31	nM	Ki	Bioorg Med Chem (2016) 24: 1619-1636 [PMID:26951894]
ChEMBL	Binding affinity to human DRD3 receptor by GTPgammaS binding assay	B	8.4	pKi	3.98	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5056-5059 [PMID:19635669]
ChEMBL	Antagonist activity at human Dopamine D3 receptor expressed in CHO cell by GTPgammaS binding assay	F	8.4	pKi	3.98	nM	Ki	J Med Chem (2010) 53: 374-391 [PMID:19891474]
ChEMBL	Antagonist activity at human dopamine D3 receptor expressed in CHO cells after 90 mins by [35S]-GTPgamma S assay	B	8.4	pKi	3.98	nM	Ki	Bioorg Med Chem Lett (2016) 26: 1329-1332 [PMID:26786693]
ChEMBL	Antagonist activity at dopamine D3 receptor by GTPgammaS binding assay	F	8.4	pKi	3.98	nM	Ki	Bioorg Med Chem Lett (2008) 18: 908-912 [PMID:18178090]
ChEMBL	Antagonist activity at human dopamine D3 receptor by cell based GTPgammaS binding assay	F	8.4	pKi	3.98	nM	Ki	Bioorg Med Chem Lett (2008) 18: 901-907 [PMID:18248991]
ChEMBL	Displacement of [35S]GTP-gamma-S from human cloned dopamine D3 receptor expressed in CHO cells after 30 mins	F	8.4	pKi	3.98	nM	Ki	J Med Chem (2007) 50: 5076-5089 [PMID:17867665]
ChEMBL	Antagonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay	F	8.4	pKi	3.98	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4799-4801 [PMID:19560918]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL	Inhibition of [125I]-iodosulpiride binding to rat Dopamine D3 receptor expressed in CHO cells	B	7.97	pKi	10.7	nM	Ki	J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
ChEMBL	Displacement of [125I]-7-OH-PIPAT from rat brain dopamine D3 receptor after 45 mins by microplate scintillation counting analysis	B	8.2	pKi	6.31	nM	Ki	Bioorg Med Chem Lett (2016) 26: 1329-1332 [PMID:26786693]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Displacement of [3H]-dofetilide from human ERG potassium channel by scintillation proximity assay	B	6.2	pKi	630.96	nM	Ki	Bioorg Med Chem Lett (2016) 26: 1329-1332 [PMID:26786693]
ChEMBL	Displacement of [3H]dofetilide from hERG expressed in CHO cells	B	5.7	pIC50	1995.26	nM	IC50	J Med Chem (2007) 50: 5076-5089 [PMID:17867665]
ChEMBL	Inhibition of human ERG	B	5.7	pIC50	1995.26	nM	IC50	Bioorg Med Chem Lett (2008) 18: 908-912 [PMID:18178090]
ChEMBL	Displacement of [3H]Dofetilide from human ERG	B	5.7	pIC50	1995.26	nM	IC50	Bioorg Med Chem Lett (2008) 18: 901-907 [PMID:18248991]
ChEMBL	Displacement of [3H]dofetilide from human ERG channel by scintillation proximity assay	B	5.7	pIC50	1995.26	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4799-4801 [PMID:19560918]
ChEMBL	Displacement of [3H]dofetilide from human ERG	B	5.7	pIC50	1995.26	nM	IC50	Bioorg Med Chem Lett (2009) 19: 5056-5059 [PMID:19635669]
ChEMBL	Displacement of [3H]dofetidile from human ERG by scintillation proximity assay	B	5.7	pIC50	1995.26	nM	IC50	J Med Chem (2010) 53: 374-391 [PMID:19891474]
ChEMBL	Inhibition of human ERG transfected in HEK293 cells assessed as reduction in tail current by patch clamp assay	B	6.17	pIC50	676.08	nM	IC50	J Med Chem (2016) 59: 8549-8576 [PMID:27564135]
ChEMBL	Inhibition of human ERG tail current expressed in HEK293 cells after 5 mins by patch clamp assay	B	6.2	pIC50	630.96	nM	IC50	Bioorg Med Chem (2016) 24: 1619-1636 [PMID:26951894]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	Antagonist activity at histamine H1 receptor by FLIPR assay	F	6.2	pKi	630.96	nM	Ki	Bioorg Med Chem Lett (2008) 18: 908-912 [PMID:18178090]
ChEMBL	Antagonist activity at histamine H1 receptor by FLIPR assay	F	6.2	pKi	630.96	nM	Ki	Bioorg Med Chem Lett (2008) 18: 901-907 [PMID:18248991]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb	-	-	5.8	pKi	-	-	-	J Pharmacol Exp Ther (2000) 294: 1154-65 [PMID:10945872]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb	-	-	5.9	pKi	-	-	-	J Pharmacol Exp Ther (2000) 294: 1154-65 [PMID:10945872]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]