rifamycin SV [Ligand Id: 4570] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL437765 (Rifamycin Sv, CB-01-11, M-14, Rifomycin, Rifamycin)
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • OATP1A2/Solute carrier organic anion transporter family member 1A2 in Human [ChEMBL: CHEMBL1743123] [GtoPdb: 1219] [UniProtKB: P46721]
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
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  • OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5]
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  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]