niflumic acid [Ligand Id: 2439] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL63323 (Niflugel, Niflumic acid, NSC-758196, UP 83, UP-83)
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  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
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  • KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3]
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  • TRPA1 in Rat [GtoPdb: 485] [UniProtKB: Q6RI86]
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  • ClC-Ka in Human [GtoPdb: 700] [UniProtKB: P51800]
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  • ClC-Kb in Human [GtoPdb: 701] [UniProtKB: P51801]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.97 pIC50 1064 nM IC50 DrugMatrix in vitro pharmacology data
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.04 pIC50 918 nM IC50 DrugMatrix in vitro pharmacology data
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
ChEMBL Inhibition of human recombinant DHODH B 4.77 pIC50 17000 nM IC50 ACS Med Chem Lett (2016) 7: 1112-1117 [PMID:27994748]
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis B 5.44 pKi 3610 nM Ki J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins B 5.89 pIC50 1280 nM IC50 ACS Med. Chem. Lett. (2012) 3: 165-169 [PMID:24900447]
ChEMBL Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay F 4.4 pEC50 40200 nM EC50 ACS Med. Chem. Lett. (2012) 3: 165-169 [PMID:24900447]
ChEMBL Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay B 4.51 pEC50 30800 nM EC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay B 4.82 pEC50 15000 nM EC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay F 5.94 pEC50 1150 nM EC50 ACS Med. Chem. Lett. (2012) 3: 165-169 [PMID:24900447]
ChEMBL Agonist activity at human GPR35 by DMR assay B 5.95 pEC50 1110 nM EC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
Transcriptional enhancer factor TEF-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295828] [UniProtKB: Q15561]
ChEMBL Binding affinity to human His-tagged TEAD4 YBD (217 to 434 residues) expressed in Escherichia coli BL21(DE3) after 30 mins by ITC assay B 4.55 pKd 28000 nM Kd J Med Chem (2018) 61: 5057-5072 [PMID:29251924]
ChEMBL Binding affinity to N-terminal His6-tagged human TEAD4 YAP binding domain (217 to 434 residues) expressed in Escherichia coli C43 (DE3) cells by ITC method B 4.55 pKd 28000 nM Kd J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
ChEMBL Inhibition of CPM binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by CPM addition and measured after 1 hr by fluorescence assay B 4.38 pIC50 41900 nM IC50 J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
ChEMBL Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay B 5.23 pIC50 5900 nM IC50 J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
Transcription factor SOX-18 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523228] [UniProtKB: P43680]
ChEMBL Inhibition of mouse SOX18 expressed in African green monkey COS7 cells assessed as reduction in SOX18 transcriptional activity by luciferase reporter gene assay B 4.3 pIC50 50500 nM IC50 WO-2018112545-A1. Inhibitors of sox18 protein activity for treating angiogenesis- and/or lymphangiogenesis-related diseases (null)
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 6.59 pKd 260 nM Kd J. Med. Chem. (2015) 58: 6507-6515 [PMID:26214366]
ChEMBL FP Assay: 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). B 6.54 pIC50 289 nM IC50 US-8877795-B2. Identification of stabilizers of multimeric proteins (2014)
KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3]
GtoPdb - - 8.68 pEC50 2.1 nM EC50 J Gen Physiol (2010) 135: 275-95 [PMID:20176855];
Mol Pharmacol (2012) 82: 795-802 [PMID:22851714]
TRPA1 in Rat [GtoPdb: 485] [UniProtKB: Q6RI86]
GtoPdb Two electrode voltage clamp - 3.3 pEC50 - - - Pflugers Arch (2010) 459: 579-92 [PMID:19888597]
ClC-Ka in Human [GtoPdb: 700] [UniProtKB: P51800]
GtoPdb - - 5 pEC50 10000 nM EC50
ClC-Kb in Human [GtoPdb: 701] [UniProtKB: P51801]
GtoPdb - - 5 pEC50 10000 nM EC50

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]