rifampicin [Ligand Id: 2765] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL374478 (Abrifam, BA 411661E, BA-41166E, Eremfat, L-5103, L-5103 LEPETIT, L-5103-LEPETIT, NIH-10782, NSC-113926, Rifadin, Rifadine, Rifaldazine, Rifaldin, Rifampicin, Rifampicinum, Rifampin, Rifamycin amp, Rifapiam, Rifaprodin, Rifoldin, Rimactan, Rimactane) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840] | ||||||||
| ChEMBL | Inhibition of human alpha-synuclein filament formation expressed in Escherichia coli BL21(DE3) cells incubated for 72 hrs by thioflavin S based fluorescence assay | B | 4.34 | pIC50 | 46200 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| ChEMBL | Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay | B | 5.15 | pIC50 | 7100 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| 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 |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique | B | 4.25 | pIC50 | 56000 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| 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: P9WG45, P9WG47] | ||||||||
| 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: Q548M1, Q7BGE6] | ||||||||
| 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: P10809, P61604] | ||||||||
| 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 | Activation of human PXR | B | 5.92 | pEC50 | 1190 | nM | EC50 | J Med Chem (2021) 64: 6413-6522 [PMID:34003642] |
| ChEMBL | Agonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as transcriptional activation incubated for 24 hrs by luminescence based analysis | B | 5.93 | pEC50 | 1170 | nM | EC50 | J Med Chem (2022) 65: 16829-16859 [PMID:36480704] |
| 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 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]
