phenoxybenzamine [Ligand Id: 7268] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL753 (Bensylyt, Benzylyt, Dibenylin, Phenoxybenzamine)
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
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  • α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.82 pIC50 15100 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells F 5.57 pIC50 2720 nM IC50 Br J Pharmacol (2002) 136: 829-836 [PMID:12110607]
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells F 5.31 pIC50 4900 nM IC50 Br J Pharmacol (2002) 136: 829-836 [PMID:12110607]
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells F 5.21 pIC50 6130 nM IC50 Br J Pharmacol (2002) 136: 829-836 [PMID:12110607]
α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 8.4 pKi - - - Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb Two site binding - 6.4 pKi - - - Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
GtoPdb - - 8.5 pKi 3.5 nM Ki J Biol Chem (1991) 266: 22427-35 [PMID:1834671]

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]