meclofenamic acid [Ligand Id: 7219] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL509 (CI-583, CL-583, INF 4668, INF-4668, Meclodium, Meclofenamate, Meclofenamic acid, Meclomen, NSC-95309)
  • 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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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • fatty acid binding protein 2/Fatty acid binding protein intestinal in Human [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 5.5 pIC50 3160 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
ChEMBL Inhibition of AKR1C1 (unknown origin) B 5.5 pIC50 3160 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
ChEMBL Inhibition of recombinant human AKR1C1 expressed in Escherichia coli BL21 cells in presence of 9,10-phenanthrenequinone and NADPH by fluorescence assay B 6.13 pIC50 740 nM IC50 Bioorg Med Chem (2018) 26: 5934-5943 [PMID:30429100]
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 5.06 pIC50 8740 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
ChEMBL Inhibition of AKR1C2 (unknown origin) B 5.06 pIC50 8740 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 N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 6.27 pIC50 540 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
ChEMBL Inhibition of AKR1C3 (unknown origin) B 6.27 pIC50 540 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
ChEMBL Inhibition of recombinant human AKR1C3 expressed in Escherichia coli BL21 cells in presence of 9,10-phenanthrenequinone and NADPH by fluorescence assay B 6.29 pIC50 512 nM IC50 Bioorg Med Chem (2018) 26: 5934-5943 [PMID:30429100]
Aldo-keto reductase family 1 member C4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
ChEMBL Inhibition of AKR1C4 (unknown origin) B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL Compound was evaluated for its inhibitory activity against 5-LO (5-lipoxygenase) B 4.62 pIC50 24000 nM IC50 Bioorg Med Chem Lett (1992) 2: 705-708
ChEMBL Compound was evaluated in an intact RBL-1 cell line for inhibition of 5-lipoxygenase B 4.62 pIC50 24000 nM IC50 Bioorg Med Chem Lett (1992) 2: 69-72
ChEMBL Inhibition 5-lipoxygenase mediated LTB4 formation in rat basophilic leukemia (RBL-1) cells B 4.62 pIC50 24000 nM IC50 J Med Chem (1993) 36: 1802-1810 [PMID:8515419]
ChEMBL Inhibition of 5-lipoxygenase measured by the reduction of leukotriene B4 (LTB4) in intact basophilic rat leukemia cells F 4.62 pIC50 24000 nM IC50 J Med Chem (1993) 36: 1090-1099 [PMID:8478906]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX1 (unknown origin) B 6.66 pIC50 220 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 6.69 pIC50 203 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb - - 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-4 [PMID:11844663]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibition of the ovine Prostaglandin G/H synthase 1 was determined by thin-layer chromatography assay B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-524 [PMID:11844663]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of COX2 (unknown origin) B 6.15 pIC50 700 nM IC50 Eur J Med Chem (2013) 62: 738-744 [PMID:23454516]
ChEMBL Inhibition of the human Prostaglandin G/H synthase 2 was determined by thin-layer chromatography assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-524 [PMID:11844663]
GtoPdb - - 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-4 [PMID:11844663]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 7.96 pIC50 11 nM IC50 DrugMatrix in vitro pharmacology data
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL Inhibition of the murine Arg120Ala mutant type COX-2 B 6.4 pIC50 400 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-524 [PMID:11844663]
ChEMBL Inhibition of the murine wild type Prostaglandin G/H synthase 2 B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2002) 12: 521-524 [PMID:11844663]
fatty acid binding protein 2/Fatty acid binding protein intestinal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP B 5.05 pKi 8900 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.42 pKi 379 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.59 pKi 256 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) B 5.5 pIC50 3144 nM IC50 DrugMatrix in vitro pharmacology data
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis B 6.32 pKd 480 nM Kd J Med Chem (2015) 58: 6507-6515 [PMID:26214366]
ChEMBL Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis B 4.3 pIC50 50000 nM IC50 J Med Chem (2015) 58: 6507-6515 [PMID:26214366]
TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
GtoPdb - - 5.47 pIC50 3420 nM IC50 Eur Heart J (2022) 43: 4195-4207 [PMID:35822895]

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]