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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
There should be some charts here, you may need to enable JavaScript!
  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
There should be some charts here, you may need to enable JavaScript!
  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
There should be some charts here, you may need to enable JavaScript!
  • Alpha-ketoglutarate-dependent dioxygenase alkB homolog 3 in Human [ChEMBL: CHEMBL3112376] [UniProtKB: Q96Q83]
There should be some charts here, you may need to enable JavaScript!
  • Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
There should be some charts here, you may need to enable JavaScript!
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • fatty acid binding protein 2/Fatty acid binding protein intestinal in Human [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
There should be some charts here, you may need to enable JavaScript!
  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
There should be some charts here, you may need to enable JavaScript!
  • Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736]
There should be some charts here, you may need to enable JavaScript!
  • Retinoid X receptor-α/Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2/Retinoic acid receptor RXR-alpha in Human [ChEMBL: CHEMBL3885613] [GtoPdb: 610, 630] [UniProtKB: P19793, P43354]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
There should be some charts here, you may need to enable JavaScript!
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]
Alpha-ketoglutarate-dependent dioxygenase alkB homolog 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3112376] [UniProtKB: Q96Q83]
ChEMBL Inhibition of human ALKBH3 demethylase activity by restriction endonuclease digestion assay B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
ChEMBL Displacement of dm6A-containing ssDNA from truncated N-terminal his-tagged human FTO (31 residues) mediated demethylation activity expressed in Escherichia coli BL21(DE3) using ssDNA (5'-ATTGTCA(dm6A)CAGCAGA-FAM-3') as substrate by fluorescence polarization assay B 4.76 pIC50 17400 nM IC50 Eur J Med Chem (2020) 196: 112325-112325 [PMID:32330741]
ChEMBL Inhibition of N-terminal 31 residues truncated His-tagged human FTO demethylase activity expressed in Escherichia coli BL21(DE3) cells B 5.1 pIC50 8000 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
ChEMBL Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis B 5.1 pIC50 7940 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
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]
DNA oxidative demethylase ALKBH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169164] [UniProtKB: Q6NS38]
ChEMBL Inhibition of human ALKBH2 demethylase activity by restriction endonuclease digestion assay B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
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
Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736]
ChEMBL Inhibition of Gal4-fused Nur77 in HEK293T cells B 5.33 pEC50 4700 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
Retinoid X receptor-α/Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2/Retinoic acid receptor RXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885613] [GtoPdb: 610, 630] [UniProtKB: P19793, P43354]
ChEMBL Inhibition of full-length Nurr1-RXRalpha in human SH-SY5Y cells B 6.05 pEC50 900 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
RNA demethylase ALKBH5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621037] [UniProtKB: Q6P6C2]
ChEMBL Inhibition of N-terminal His-tagged human ALKBH5 (66 to 292 residues) B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
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 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]