trans-flupenthixol [Ligand Id: 968] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL42055 (.beta.-flupenthixol, E-flupenthixol, E-flupentixol, Flupenthixol, Flupentixol, (e)-, Flupentixole, Trans-flupenthixol, Trans-flupentixol)
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined B 7.74 pKi 18 nM Ki J Med Chem (1997) 40: 952-960 [PMID:9083484]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate B 7.42 pKi 37.8 nM Ki J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL The compound was tested for affinity towards sigma-3 receptor B 7.83 pIC50 14.79 nM IC50 J Med Chem (1994) 37: 4109-4117 [PMID:7990111]
D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 6.92 pKi 120 nM Ki J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]
D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 6.52 pKi 300 nM Ki J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]

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]