efonidipine [Ligand Id: 12565] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2074922 (Efonidipine, Efonidipine hydrochloride)
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  • Cav3.2 in Human [GtoPdb: 536] [UniProtKB: O95180]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (+)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells F 4.69 pIC50 20600 nM IC50 Pharm Res (2000) 17: 1189-1197 [PMID:11145223]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (-)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells F 4.76 pIC50 17300 nM IC50 Pharm Res (2000) 17: 1189-1197 [PMID:11145223]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells F 4.89 pIC50 13000 nM IC50 Eur J Pharm Sci (2002) 16: 159-165 [PMID:12128170]
Cav3.2 in Human [GtoPdb: 536] [UniProtKB: O95180]
GtoPdb - - 6.4 pIC50 - - - Pharmacology (2006) 78: 11-20 [PMID:16899990]

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]