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ChEMBL ligand: CHEMBL753 (Bensylyt, Benzylyt, Dibenylin, Phenoxybenzamine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]