S33084 [Ligand Id: 129] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL65280
  • 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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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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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 Ability to displace [125I]iodosulpiride from human dopamine D2 (hD2) receptor transfected into CHO cells. B 7.5 pKi 31.62 nM Ki Bioorg Med Chem Lett (1999) 9: 2059-2064 [PMID:10450981]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 6.69 pKi 205 nM Ki Med Chem Res (2004) 13: 25-33
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity for human Dopamine receptor D3 B 8.6 pKi 8.6 nM Log Ki J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
ChEMBL Ability to displace [125I]iodosulpiride from human dopamine D3 (hD3) receptor transfected into CHO cells. B 9.5 pKi 0.32 nM Ki Bioorg Med Chem Lett (1999) 9: 2059-2064 [PMID:10450981]
GtoPdb - - 9.6 pKi 0.25 nM Ki J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL 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 counting B 8.62 pKi 2.42 nM Ki Med Chem Res (2004) 13: 25-33
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.1 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 6.9 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.8 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 7.1 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]

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]