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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 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]