tolfenamic acid [Ligand Id: 8769] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL121626 (Clotam, Clotam rapid, N-(3-chloro-o-tolyl)anthranilic, NSC-757873, Tolfenamic acid)
  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Inhibition of human AKR1C3 using S-(+)-1,2,3,4-tetrahydro-1-naphthol as substrate B 8.1 pKi 8 nM Ki J Nat Prod (2012) 75: 716-721 [PMID:22506594]
GtoPdb - - 8.1 pKi 8 nM Ki J Biol Chem (2007) 282: 8368-79 [PMID:17166832]
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction after 2 hrs by fluorescence polarization assay B 4.33 pIC50 47000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 16074-16079 [PMID:17911242]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated 10 mins followed by substrate addition and measured after 2 mins by ELISA B 6.06 pIC50 880 nM IC50 Eur J Med Chem (2021) 226: 113817-113817 [PMID:34537445]
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 6.82 pKd 150 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 4.4 pIC50 40000 nM IC50 J Med Chem (2015) 58: 6507-6515 [PMID:26214366]

ChEMBL data shown on this page come from version 33:

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]