meclofenamic acid [Ligand Id: 7219] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL509 (Acide meclofenamique, Acido meclofenamico, CI-583, CL-583, INF 4668, INF-4668, Meclofenamate, Meclofenamic acid, NSC-95309) |
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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] |
| 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] |
| 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/Mitogen-activated protein kinase 1 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 |
| methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/N6-adenosine-methyltransferase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739695] [GtoPdb: 3181] [UniProtKB: Q86U44] | ||||||||
| ChEMBL | Inhibition of METTL3 (unknown origin) | B | 5.1 | pIC50 | 8000 | nM | IC50 | Eur J Med Chem (2024) 274: 116526-116526 [PMID:38805939] |
| 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] |
| Nerve Growth factor IB/Nuclear receptor subfamily 4immunitygroup 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] |
| 5-LOX/Polyunsaturated fatty acid 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 /Prostaglandin G/H synthase 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] |
| Prostaglandin G/H synthase 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 /Prostaglandin G/H synthase 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 /Prostaglandin G/H synthase 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] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Displacement of carboxyfluorescein-labelled bbc3-(dG)14 from SARS-CoV-2 Mac3 by fluorescence polarization analysis | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2022) 65: 15227-15237 [PMID:36356292] |
| 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] |
| ChEMBL | Fluorescence Polarization Binding Assay: Table 3: The FP assay was then adapted for HTS and used to screen 120,000 small molecule library for compounds that displaced probe 5 from the T4 binding of TTR. The FP assay was performed in 384-well plate using very low concentration of probe 5 (1.5 nM) and TTR (50 nM) in a 10 μL assay volume. A detergent (0.01% Triton-X100) was added to the assay buffer to avoid any false positive hits from promiscuous, aggregate-based inhibitors. The assay demonstrated robust performance, with a very good dynamic range (70-230 mP) and a Z′ factor in the range of 0.57-0.78 (FIGS. 4A and 4B). Hits were defined as compounds that resulted in at least 50% decrease in fluorescence polarization and demonstrated relative fluorescence between 70 and 130%. Many fluorescence quenchers and enhancers having less than 70% and greater than 130% total fluorescence relative to a control, respectively, were excluded from the hit list. 200 compounds were designated as positive hits (0.167% hit rate). The 200 hits were then evaluated in a dose-response manner and their IC50 (compound concentration that resulted in 50% decrease in the FP signal) values were determined. Among the 200 compounds screened, 33 compounds showed a dose-response effect on the FP and displayed IC50≤10 μM. | B | 6.3 | pIC50 | 504 | nM | IC50 | US-11337935-B2. Identification of stabilizers of multimeric proteins (2022) |
| 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 36:
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]
