dilazep [Ligand Id: 4717] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL126075 (Dilazep, Dilazep dihydrochloride)
  • Equilibrative nucleoside transporter 1 in Human [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808]
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  • ABCC4/Multidrug resistance-associated protein 4 in Human [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
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  • ABCC5/Multidrug resistance-associated protein 5 in Human [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Equilibrative nucleoside transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808]
GtoPdb - - 9 pKi 1 nM Ki
ChEMBL Inhibition of human ENT1 expressed in porcine PK15NTD cells by cell-based [3H]5-uridine uptake assay B 7.76 pIC50 17.5 nM IC50 Bioorg Med Chem Lett (2014) 24: 5801-5804 [PMID:25454272]
Equilibrative nucleoside transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287614] [GtoPdb: 1118] [UniProtKB: O54699]
ChEMBL Inhibition of rat ENT2 expressed in rat H9c2 cells by cell-based 3H[5-]uridine uptake assay B 5.06 pIC50 8800 nM IC50 Bioorg Med Chem Lett (2014) 24: 5801-5804 [PMID:25454272]
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
ChEMBL TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells F 4.7 pIC50 20000 nM IC50 Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538]
ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440]
ChEMBL TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells F 4.3 pIC50 >50000 nM IC50 Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538]

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]