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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]