mefenamic acid [Ligand Id: 2593] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL686 (CI-473, CN-35355, Contraflam, Dysman-250, Dysman-500, Gardan, INF-3355, J2.344B, M01AG01, Mefenamate, Mefenamic acid, Mefenaminic acid, Meflam 250, Meflam 500, Mendys, Mephenamic acid, Mephenaminic acid, NSC-94437, Opustan 250, Opustan 500, Ponstan, Ponstan fte, Ponstel)
  • Acetylcholinesterase in Torpedo californica [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
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  • Aldo-keto reductase family 1 member B10 in Human [ChEMBL: CHEMBL5983] [UniProtKB: O60218]
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  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
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  • aldo-keto reductase family 1 member B/Aldose reductase in Human [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
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  • dihydrofolate reductase/Dihydrofolate reductase in Human [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374]
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  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
ChEMBL Inhibition of Torpedo californica eel AChE using acetylthiocholine/DTNB as substrate assessed as ROS-induced enzyme inactivation preincubated for 10 mins followed by substrate addition measured every 30 secs for 20 mins in presence of horseradish peroxidase and H2O2 B 5.21 pIC50 6120 nM IC50 Medchemcomm (2011) 2: 406-412
Aldo-keto reductase family 1 member B10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5983] [UniProtKB: O60218]
ChEMBL Inhibition of wild-type N-terminal 6-His tagged AKR1B10 (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as pyridine-3-aldehyde reduction by spectrophotometry B 5.8 pIC50 1600 nM IC50 J Med Chem (2015) 58: 2047-2067 [PMID:25375908]
Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
ChEMBL Inhibition of human recombinant AKR1C1 assessed as 1-acenaphthenol oxidation by spectrophotometry B 6.09 pKi 810 nM Ki J Med Chem (2012) 55: 7417-7424 [PMID:22881866]
ChEMBL Inhibition of AKR1C1 (unknown origin) B 5.41 pIC50 3910 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
ChEMBL Inhibition of human recombinant AKR1C2 assessed as 1-acenaphthenol oxidation by spectrophotometry B 6.66 pKi 220 nM Ki J Med Chem (2012) 55: 7417-7424 [PMID:22881866]
ChEMBL Inhibition of AKR1C2 (unknown origin) B 5.16 pIC50 6970 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Inhibition of human recombinant AKR1C3 assessed as 1-acenaphthenol oxidation by spectrophotometry B 6.52 pKi 300 nM Ki J Med Chem (2012) 55: 7417-7424 [PMID:22881866]
ChEMBL Inhibition of AKR1C3 (unknown origin) B 6.25 pIC50 560 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
Aldo-keto reductase family 1 member C4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
ChEMBL Inhibition of AKR1C4 (unknown origin) B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
ChEMBL Inhibition of human AR by fluorescence assay B 4.11 pIC50 77000 nM IC50 J Med Chem (2015) 58: 2047-2067 [PMID:25375908]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
GtoPdb - - 4.6 pIC50 25000 nM IC50 Eur J Med Chem (2013) 62: 738-44 [PMID:23454516]
ChEMBL Inhibition of COX1 (unknown origin) B 4.6 pIC50 25000 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 6.94 pIC50 116 nM IC50 DrugMatrix in vitro pharmacology data
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of COX2 (unknown origin) B 5.54 pIC50 2900 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
GtoPdb - - 5.54 pIC50 2900 nM IC50 Eur J Med Chem (2013) 62: 738-44 [PMID:23454516]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.22 pIC50 602 nM IC50 DrugMatrix in vitro pharmacology data
dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374]
ChEMBL Inhibition of human DHFR in presence of DHF and NADPH by UV-vis spectrometry by Lineweaver-Burk plot analysis B 4.14 pKi 72000 nM Ki J Med Chem (2020) 63: 8314-8324 [PMID:32658475]
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of recombinant MPO (unknown origin) assessed as reduction in LDL oxidation in presence of H2O2 and HCl after 5 mins by ELISA B 5.66 pIC50 2210 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
ChEMBL Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins B 6.01 pIC50 980 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-primed C57BL/6 mouse bone marrow derived macrophages preincubated for 15 mins followed by addition of ATP and measured after 1 hr by ELISA B 4.6 pIC50 25000 nM IC50 Eur J Med Chem (2020) 185: 111822-111822 [PMID:31699536]
Nicotinate phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523354] [UniProtKB: Q6XQN6]
ChEMBL Inhibition of NAPRT (unknown origin) B 10.3 pKi 0.05 nM Ki WO-2017162840-A1. Sensitization of cancer cells to nampt inhibitors by nicotinic acid phosphoribosyltransferase neutralization (null)
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL Agonist activity at human TRPA1 in WI38 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay B 4.21 pEC50 61000 nM EC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay B 4.78 pEC50 16595.87 nM EC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay B 4.8 pEC50 16000 nM EC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]

ChEMBL data shown on this page come from version 32:

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]