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Assay Detail

CHEMBL5261221

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Binding
Inhibition of wild type human IDH1 measured after 2 hrs in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS.
ACS Med Chem Lett (2017) 8 : 151 -156
PubMed 28197303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.93 5.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3677013 1 5.99
CHEMBL4169151 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3677013 IC50 = 1030.0 nM 5.99
CHEMBL4169151 IC50 = 1380.0 nM 5.86