SB 277011-A [Ligand Id: 143] activity data from GtoPdb and ChEMBL

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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]
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  • 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]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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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 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]