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Assay Detail

CHEMBL4628664

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of IDH1 R132C mutant (unknown origin)
7
Total Activities
7
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

Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.
Li Z, Wu X, Jia L, Li J, Zhang R, Tang H, Li Z, Bu H, Shen C.
Bioorg Med Chem Lett (2020) 30 : 127070 -127070
PubMed 32143887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.41 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180727 1 6.41
CHEMBL3989908 ENASIDENIB 4.0 1 -
CHEMBL3392845 1 -
CHEMBL4643441 1 -
CHEMBL4646777 1 -
CHEMBL4634103 1 -
CHEMBL4639434 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180727 IC50 = 390.0 nM 6.41
CHEMBL3989908 ENASIDENIB IC50 > 100000.0 nM -
CHEMBL3392845 IC50 > 100000.0 nM -
CHEMBL4643441 IC50 > 100000.0 nM -
CHEMBL4646777 IC50 > 100000.0 nM -
CHEMBL4634103 IC50 > 100000.0 nM -
CHEMBL4639434 IC50 > 100000.0 nM -