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) |
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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] |
| Cytochrome c oxidase subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6174] [UniProtKB: P00403] | ||||||||
| ChEMBL | Inhibition of human COX-2 assessed as by fluorescence based microplate reader assay | B | 5.85 | pIC50 | 1410 | nM | IC50 | J Med Chem (2022) 65: 10481-10505 [PMID:35868003] |
| ChEMBL | Inhibition of COX-2 (unknown origin) | B | 5.93 | pIC50 | 1170 | nM | IC50 | Eur J Med Chem (2022) 240: 114560-114560 [PMID:35777102] |
| 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 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]
