etodolac [Ligand Id: 7185] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL622 (AY-24,236, AY-24-236, AY-24236, Ebretin, Eccoxolac, Edolan, Etodolac, Etodolic acid, Etolyn, Etopan xl, Flancox, Lodine, Lodine sr, Lodine xl, Lodin xl, Napilac, NIH-9918, NSC-282126, Ramodar, (rs)-etodolic acid, Tedolan, Ultradol, Zedolac)
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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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 Inhibition of COX1 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production by radioimmunoassay B 4.99 pIC50 10300 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.58 pIC50 2649 nM IC50 DrugMatrix in vitro pharmacology data
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
GtoPdb Measured as LPS-induced PGE2 production in COX-1-inhibited human monocytes. - 4.28 pIC50 53000 nM IC50 J Pharm Pharmacol (2001) 53: 1679-85 [PMID:11804398]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay B 5.7 pIC50 2000 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.25 pIC50 561 nM IC50 DrugMatrix in vitro pharmacology data
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 4.3 pIC50 50000 nM IC50 J Pharmacol Exp Ther (2000) 295: 10-15 [PMID:10991954]
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
ChEMBL Inhibition of rat Oat1 expressed in pig LLC-PK11 cells B 4 pKi >100000 nM Ki Bioorg Med Chem (2011) 19: 3320-3340 [PMID:21571536]

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]