diflunisal [Ligand Id: 7162] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL898 (Diflunisal, Dolobid 500, Dolobid)
  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of human carbonic anhydrase 1 esterase activity by noncompetitive Lineweaver-Burke plot B 5.07 pKi 8450 nM Ki Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
ChEMBL Inhibition of human carbonic anhydrase 1 esterase activity by spectrophotometry B 5.47 pIC50 3380 nM IC50 Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of human carbonic anhydrase 2 esterase activity by non-competitive Lineweaver-Burke plot B 5.03 pKi 9370 nM Ki Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
ChEMBL Inhibition of human carbonic anhydrase 2 esterase activity by spectrophotometry B 5.57 pIC50 2700 nM IC50 Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
ChEMBL TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells F 6.07 pIC50 850 nM IC50 J. Pharmacol. Exp. Ther. (2000) 295: 10-15 [PMID:10991954]
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 6.24 pKd 580 nM Kd J. Med. Chem. (2015) 58: 6507-6515 [PMID:26214366]
ChEMBL Binding affinity to transthyretin (unknown origin) by ITC method B 6.39 pKd 407 nM Kd J Med Chem (2018) 61: 7862-7876 [PMID:30133284]
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 4.6 pIC50 25000 nM IC50 J. Med. Chem. (2015) 58: 6507-6515 [PMID:26214366]
ChEMBL Inhibition of TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as inhibition of amyloid fibril formation by fluorescence assay B 5.25 pEC50 5600 nM EC50 J. Med. Chem. (2014) 57: 8928-8935 [PMID:25314129]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]