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ChEMBL ligand: CHEMBL1086218 (Amdray, PSC 833, SDZ PSC 833, SDZ-PSC 833, Valspodar) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells | F | 4.54 | pKi | 28900 | nM | Ki | Mol Pharmacol (1999) 56: 1219-1228 [PMID:10570049] |
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells | F | 4.57 | pKi | 27000 | nM | Ki | J Biol Chem (1994) 269: 27807-27810 [PMID:7961706] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in CEM/VBL 100 cells | F | 5.89 | pKi | 1300 | nM | Ki | Biochem Biophys Res Commun (1999) 257: 410-413 [PMID:10198227] |
GtoPdb | - | - | 5.89 | pKi | 1300 | nM | Ki | Biochem Biophys Res Commun (1999) 257: 410-3 [PMID:10198227] |
ChEMBL | TP_TRANSPORTER: inhibition of ATPase activity (Verapamil) in P-gp-MRP-16-Protein A complex | F | 6.87 | pKi | 134 | nM | Ki | Br J Pharmacol (1997) 122: 241-248 [PMID:9313931] |
ChEMBL | TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) (Vinblastine: 0.1 uM) in MDR1-expressing LLC-PK1 cells | F | 5.97 | pIC50 | 1060 | nM | IC50 | Jpn J Cancer Res (1998) 89: 1220-1228 [PMID:9914792] |
ChEMBL | Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis | B | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (2012) 55: 3261-3273 [PMID:22452412] |
ChEMBL | TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Doxorubicin: 0.8 uM) in MDR1-expressing LLC-PK1 cells | F | 6.54 | pIC50 | 291 | nM | IC50 | Jpn J Cancer Res (1998) 89: 1220-1228 [PMID:9914792] |
ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 6.96 | pIC50 | 110 | nM | IC50 | Drug Metab Dispos (2000) 28: 655-660 [PMID:10820137] |
ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells | F | 7.65 | pIC50 | 22.2 | nM | IC50 | Drug Metab Dispos (2000) 28: 1238-1243 [PMID:10997946] |
ChEMBL | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells | F | 6.39 | pEC50 | 410 | nM | EC50 | Anticancer Drugs (1996) 7: 568-578 [PMID:8862725] |
ChEMBL | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-P388 cells | F | 6.96 | pEC50 | 110 | nM | EC50 | Anticancer Drugs (1996) 7: 568-578 [PMID:8862725] |
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]