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ChEMBL ligand: CHEMBL85606 (SB-277011) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]