rifampicin [Ligand Id: 2765] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL374478 (Eremfat, L-5103-LEPETIT, NSC-113926, L-5103, BA 411661E, BA-41166E, L-5103 LEPETIT, NIH-10782, Rimactane, Rifamycin amp, Rifadin, Rifampin, Rifampicin)
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
  • This target only has 0 pki data point
  • 0
1 CHEMBL374478_lig_chart_1 Arachidonate 15-lipoxygenase Rabbit
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  • ABCB11/Bile salt export pump in Human [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
  • ABCB11/Bile salt export pump in Rat [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127]
  • This target only has 1 pki data point
  • 4.92
2 CHEMBL374478_lig_chart_2 Bile salt export pump HumanRat
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  • Caspase 1/Caspase-1 in Human [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466]
  • This target only has 0 pki data point
  • 0
3 CHEMBL374478_lig_chart_3 Caspase-1 Human
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  • CYP51A1/Cytochrome P450 51 in Human [ChEMBL: CHEMBL3849] [GtoPdb: 1374] [UniProtKB: Q16850]
  • This target only has 0 pki data point
  • 0
4 CHEMBL374478_lig_chart_4 Cytochrome P450 51 Human
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  • DNA-directed RNA polymerase beta chain in Mycobacterium tuberculosis [ChEMBL: CHEMBL2006] [UniProtKB: P9WGY9]
  • This target only has 0 pki data point
  • 0
5 CHEMBL374478_lig_chart_5 DNA-directed RNA polymerase beta chain Mycobacterium tuberculosis
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  • DNA gyrase subunit A/DNA gyrase subunit B in Mycobacterium tuberculosis [ChEMBL: CHEMBL3430898] [UniProtKB: P9WG45P9WG47]
  • This target only has 0 pki data point
  • 0
6 CHEMBL374478_lig_chart_6 DNA gyrase subunit A/DNA gyrase subunit B Mycobacterium tuberculosis
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  • Enoyl-[acyl-carrier-protein] reductase in Mycobacterium tuberculosis [ChEMBL: CHEMBL1849] [UniProtKB: P9WGR1]
  • This target only has 0 pki data point
  • 0
7 CHEMBL374478_lig_chart_7 Enoyl-[acyl-carrier-protein] reductase Mycobacterium tuberculosis
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  • glutathione S-transferase omega 1/Glutathione transferase omega 1 in Human [ChEMBL: CHEMBL3174] [GtoPdb: 3110] [UniProtKB: P78417]
  • This target only has 0 pki data point
  • 0
8 CHEMBL374478_lig_chart_8 Glutathione transferase omega 1 Human
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  • GroEL/GroES in Escherichia coli [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1Q7BGE6]
  • This target only has 0 pki data point
  • 0
9 CHEMBL374478_lig_chart_9 GroEL/GroES Escherichia coli
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10 CHEMBL374478_lig_chart_10 HSP60/HSP10 Human
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  • NH(3)-dependent NAD(+) synthetase in Bacillus subtilis (strain 168) [ChEMBL: CHEMBL4615] [UniProtKB: P08164]
  • This target only has 0 pki data point
  • 0
11 CHEMBL374478_lig_chart_11 NH(3)-dependent NAD(+) synthetase Bacillus subtilis (strain 168)
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
12 CHEMBL374478_lig_chart_12 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium yoelii [ChEMBL: CHEMBL612889]
  • This target only has 0 pki data point
  • 0
13 CHEMBL374478_lig_chart_13 Plasmodium yoelii Plasmodium yoelii
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  • Pregnane X receptor in Human [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
  • This target only has 0 pki data point
  • 0
14 CHEMBL374478_lig_chart_14 Pregnane X receptor Human
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
  • This target only has 1 pki data point
  • 4.74
15 CHEMBL374478_lig_chart_15 Solute carrier organic anion transporter family member 1A1 Rat
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  • OATP1A2/Solute carrier organic anion transporter family member 1A2 in Human [ChEMBL: CHEMBL1743123] [GtoPdb: 1219] [UniProtKB: P46721]
  • 4.29
16 CHEMBL374478_lig_chart_16 Solute carrier organic anion transporter family member 1A2 Human
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
  • 5.84
17 CHEMBL374478_lig_chart_17 Solute carrier organic anion transporter family member 1A4 Rat
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
  • 5.36
18 CHEMBL374478_lig_chart_18 Solute carrier organic anion transporter family member 1B1 Human
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  • OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5]
  • This target only has 1 pki data point
  • 5.3
19 CHEMBL374478_lig_chart_19 Solute carrier organic anion transporter family member 1B3 Human
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  • Thiosulfate sulfurtransferase in Human [ChEMBL: CHEMBL4295835] [UniProtKB: Q16762]
  • This target only has 0 pki data point
  • 0
20 CHEMBL374478_lig_chart_20 Thiosulfate sulfurtransferase Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.53 pIC50 2949 nM IC50 DrugMatrix in vitro pharmacology data
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 4.95 pIC50 11300 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 4.92 pKi 11900 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 4.46 pIC50 34700 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466]
ChEMBL DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC) B 5.08 pIC50 8319 nM IC50 DrugMatrix in vitro pharmacology data
CYP51A1/Cytochrome P450 51 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3849] [GtoPdb: 1374] [UniProtKB: Q16850]
ChEMBL Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay B 4.52 pIC50 30000 nM IC50 Drug Metab. Dispos. (2007) 35: 493-500 [PMID:17194716]
DNA-directed RNA polymerase beta chain in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2006] [UniProtKB: P9WGY9]
ChEMBL Inhibition of wild type Mycobacterium tuberculosis RNA polymerase after 10 mins using ribo green staining by rolling circle transcription assay B 2.4 pIC50 -2.4 - logIC50 Bioorg. Med. Chem. Lett. (2011) 21: 6094-6099 [PMID:21903392]
ChEMBL Inhibition of wild type Mycobacterium tuberculosis RNA polymerase after 10 mins using ribo green staining by rolling circle transcription assay B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6094-6099 [PMID:21903392]
DNA gyrase subunit A/DNA gyrase subunit B in Mycobacterium tuberculosis (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430898] [UniProtKB: P9WG45P9WG47]
ChEMBL Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis B 4.3 pIC50 >50000 nM IC50 Bioorg. Med. Chem. (2016) 24: 877-885 [PMID:26787274]
Enoyl-[acyl-carrier-protein] reductase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1849] [UniProtKB: P9WGR1]
ChEMBL Inhibition of Mycobacterium tuberculosis InhA using NADH and dodecyl coA substrate by LC-MS/MS method B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2014) 57: 6572-6582 [PMID:24967731]
glutathione S-transferase omega 1/Glutathione transferase omega 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3174] [GtoPdb: 3110] [UniProtKB: P78417]
ChEMBL Inhibition of GSTO1-1 (unknown origin) by enzymatic assay B 4.12 pIC50 75000 nM IC50 J Med Chem (2018) 61: 7448-7470 [PMID:29652143]
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1Q7BGE6]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured MDH refolding after 20 to 40 mins by spectrometric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 10651-10664 [PMID:30392371]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding after 45 mins by spectrometric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 10651-10664 [PMID:30392371]
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809P61604]
ChEMBL Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding after 40 to 60 mins by spectrometric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 10651-10664 [PMID:30392371]
NH(3)-dependent NAD(+) synthetase in Bacillus subtilis (strain 168) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4615] [UniProtKB: P08164]
ChEMBL Inhibitory activity against Bacillus subtilis NAD synthetase B 6 pIC50 >1000 nM IC50 J. Med. Chem. (2003) 46: 3371-3381 [PMID:12852767]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 48 hrs F 5.38 pIC50 4200 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 307-316 [PMID:17060533]
ChEMBL Antimalarial activity as 2nd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs by flow cytometry F 5.52 pIC50 2990 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 3485-3490 [PMID:17698630]
ChEMBL Antimalarial activity as 3rd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs dose then 48 hrs drug-free F 5.55 pIC50 2830 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 3485-3490 [PMID:17698630]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 6 pIC50 1000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity as 3rd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs dose then 48 hrs drug-free F 6.28 pIC50 528 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 3485-3490 [PMID:17698630]
ChEMBL Antimalarial activity as 2nd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by flow cytometry F 6.56 pIC50 274 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 3485-3490 [PMID:17698630]
ChEMBL Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 96 hrs F 6.72 pIC50 190 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 307-316 [PMID:17060533]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL Antimalarial activity against liver stages of Plasmodium yoelii 17XNL expressing GFP infected in human HepG2 cells transfected with CD81 assessed as growth inhibition of hepatic parasite after 40 hrs by flow cytometry F 4.65 pIC50 22200 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay B 5.64 pEC50 2300 nM EC50 J. Med. Chem. (2012) 55: 3814-3826 [PMID:22452568]
ChEMBL Agonist activity at VP16-fused human PXR expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay B 5.7 pEC50 2000 nM EC50 Bioorg Med Chem (2018) 26: 4493-4501 [PMID:30077610]
ChEMBL Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay B 5.96 pEC50 1100 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 1817-1820 [PMID:26905831]
GtoPdb - - 6 pEC50 - - - Genes Dev (1998) 12: 3195-205 [PMID:9784494];
J Clin Invest (1998) 102: 1016-23 [PMID:9727070]
ChEMBL Activation of PXR in human LS180 cells assessed as P-gp induction by measuring intracellular accumulation of rhodamine 123 preincubated for 48 hrs followed by rhodamine 123 addition after 40 mins and measured after 90 mins by fluorescence assay B 6.65 pEC50 226 nM EC50 MedChemComm (2016) 7: 1910-1915
ChEMBL Agonist activity at PXR expressed in human HepG2 cells after 24 hrs by p3A4-luciferase reporter gene assay B 6.72 pEC50 190 nM EC50 J. Med. Chem. (2016) 59: 4601-4610 [PMID:27145071]
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 Oatp1-expressing LLC-PK1 cells F 4.74 pKi 18200 nM Ki Pharm. Res. (2002) 19: 147-153 [PMID:11883641]
OATP1A2/Solute carrier organic anion transporter family member 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743123] [GtoPdb: 1219] [UniProtKB: P46721]
GtoPdb - - 4.29 pKi 51000 nM Ki Hepatology (2002) 36: 164-72 [PMID:12085361]
ChEMBL TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes F 4.29 pKi 51000 nM Ki Hepatology (2002) 36: 164-172 [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 Digoxin uptake in Oatp2-expressing LLC-PK1 cells F 5.84 pKi 1460 nM Ki Pharm. Res. (2002) 19: 147-153 [PMID:11883641]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Xenopus laevis oocytes F 5.85 pKi 1400 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 4.77 pKi 17000 nM Ki Hepatology (2002) 36: 164-172 [PMID:12085361]
GtoPdb Inhibition of atorvastatin transport by OATP1B1. - 5.96 pKi 1100 nM Ki J Med Chem (2012) 55: 4740-63 [PMID:22541068]
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 5.3 pKi 5000 nM Ki Hepatology (2002) 36: 164-172 [PMID:12085361]
GtoPdb - - 5.8 pIC50 1600 nM IC50 Drug Metab Dispos (2007) 35: 1400-7 [PMID:17496208];
J Med Chem (2012) 55: 4740-63 [PMID:22541068]
Thiosulfate sulfurtransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295835] [UniProtKB: Q16762]
ChEMBL Inhibition of refolded rhodanese (unknown origin) preincubated with Escherichia coli GroEL/GroES for 60 mins in absence of compound followed by compound addition by spectrometric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 10651-10664 [PMID:30392371]

ChEMBL data shown on this page come from version 28:

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]