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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]