compound 3 [PMID: 21650226] [Ligand Id: 8745] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1800139 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| HPGD/15-hydroxyprostaglandin dehydrogenase [NAD+] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293255] [GtoPdb: 1384] [UniProtKB: P15428] | ||||||||
| ChEMBL | Inhibition of human 15-PGDH expressed in Escherichia coli using PGE2 as substrate and NAD+ as coenzyme assessed as formation of NADH by spectrophotometric analysis | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2011) 54: 5260-5264 [PMID:21650226] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2011) 54: 5260-4 [PMID:21650226] |
| ChEMBL | Inhibition Assay: Experimental was performed by measuring the formation of NADH at 340 nm with a fluorescence spectrophotometer. Specifically, 2 ml (in total) of the solution containing 50 mM Tris-HCl (pH 7.5), 0.1 mM DTT, 0.25 mM NAD+, 10 μg of purified 15-PGDH enzyme, 21 μM PGE2 and various concentrations (0.0001 μM to 64 μM) of the derivatives according to the present invention was added to each cell. The absorbance of the reaction mixture was recorded at 340 nm so that the activities of the derivatives according to the present invention as 15-PGDH inhibitors were determined from a standard curve prepared from the absorbance of various concentrations of NADH at 340 nm. | B | 8.14 | pIC50 | 7.2 | nM | IC50 | US-8637558-B2. Thiazolidinedione derivative and use thereof (2014) |
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]
