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ChEMBL ligand: CHEMBL437765 (CB-01-11, M-14, Rifamicine sv, Rifamycin, Rifamycin Sv, Rifomycin, Rifomycin sv) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake(Rifampicin SV 30uM, 50 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus | F | 4.51 | pKi | 31000 | nM | Ki | Gastroenterology (2002) 123: 1649-1658 [PMID:12404239] |
ChEMBL | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) | F | 4.91 | pIC50 | 12200 | nM | IC50 | Pharm Res (2003) 20: 537-544 [PMID:12739759] |
ChEMBL | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 5.2 | pIC50 | 6300 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells | F | 5.42 | pKi | 3800 | nM | Ki | Gastroenterology (2000) 118: 422-430 [PMID:10648470] |
ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 5.51 | pIC50 | 3100 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 6.26 | pIC50 | 550 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
Solute carrier organic anion transporter family member 1A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781859] [UniProtKB: P46720] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in Xenopus laevis oocytes | F | 5.18 | pKi | 6600 | nM | Ki | Hepatology (2000) 32: 82-86 [PMID:10869292] |
OATP1A2/Solute carrier organic anion transporter family member 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743123] [GtoPdb: 1219] [UniProtKB: P46721] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes | F | 4.96 | pKi | 11000 | nM | Ki | Hepatology (2002) 36: 164-172 [PMID:12085361] |
GtoPdb | - | - | 4.96 | pKi | 11000 | nM | Ki | Hepatology (2002) 36: 164-72 [PMID:12085361] |
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in Xenopus laevis oocytes | F | 5.14 | pKi | 7300 | nM | Ki | Hepatology (2000) 32: 82-86 [PMID:10869292] |
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes | F | 5.7 | pKi | 2000 | nM | Ki | Hepatology (2002) 36: 164-172 [PMID:12085361] |
GtoPdb | - | - | 5.7 | pKi | 2000 | nM | Ki | Hepatology (2002) 36: 164-72 [PMID:12085361] |
ChEMBL | TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells | F | 6.64 | pIC50 | 230 | nM | IC50 | Drug Metab Dispos (2005) 33: 537-546 [PMID:15616150] |
OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes | F | 5.52 | pKi | 3000 | nM | Ki | Hepatology (2002) 36: 164-172 [PMID:12085361] |
OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes | F | 5.52 | pKi | 3000 | nM | Ki | Hepatology (2002) 36: 164-172 [PMID:12085361] |
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]