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ChEMBL ligand: CHEMBL2263632 (Aslan-003, Aslan003, ASLAN-003, ASLAN003, Farudodstat) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127] | ||||||||
ChEMBL | Inhibition of human DHODH using dihydroorotate substrate preincubated for 30 mins followed by substrate addition by DCIP based microplate reader analysis | B | 7.36 | pIC50 | 44 | nM | IC50 | J Med Chem (2021) 64: 18175-18192 [PMID:34905371] |
ChEMBL | Inhibition of human recombinant N-terminal GST-tagged DHODH expressed in Escherichia coli BL21(DE3) using dihydroorotate substrate preincubated for 5 mins followed by substrate addition by DCIP assay | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2021) 64: 5404-5428 [PMID:33844533] |
GtoPdb | - | - | 7.46 | pIC50 | 35 | nM | IC50 | Haematologica (2020) 105: 2286-2297 [PMID:33054053] |
ChEMBL | Inhibition of Homo sapiens (human) dehydroorotate dihydrogenase using 2,6-dichlorophenol-indophenol as substrate after 10 min by spectrophotometric analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | Med Chem Res (2012) 21: 3021-3034 |
ChEMBL | Inhibition Assay: DHODH activity and its inhibition were studied using a chromogen reduction assay with DCIP (2,6-dichlorophenol-indophenol). The substrate oxidation (Dihydroorotate, L-DHO), as well as cosubstrate reduction (coenzyme Q, CoQ) is coupled to the chromogen reduction, hence enzymatic activity results in a loss of chromogen absorbance at 600 nm. Enzyme extracts (8 μl, 1.5 μg of human protein) were incubated in 96-well plates. The assay mixture (200 μl) contained 200 μM CoQD, 100 μM L-DHO, 120 μM DCIP in the assay buffer (100 mM HEPES pH 8.0, 150 mM NaCl, 10% Glicerol, 0.05% Triton X-100) and 2 μl of test compound. The compounds were dissolved in DMSO at a stock concentration of 1 mM, and tested at different concentrations varying from 10 μM to 1 μM to calculate an IC50 (concentration of inhibitor required for 50% of inhibition). | B | 7.82 | pIC50 | 15 | nM | IC50 | US-8691852-B2. Amino nicotinic and isonicotinic acid derivatives as DHODH inhibitors (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]