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Assay Detail

CHEMBL4309387

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Binding
Inhibition of IDH1 R132H mutant (unknown origin) using alpha-KG as substrate after 90 mins
4
Total Activities
4
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

Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
Ma T, Zou F, Pusch S, Xu Y, von Deimling A, Zha X.
J Med Chem (2018) 61 : 8981 -9003
PubMed 29847930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.13 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463644 1 8.70
CHEMBL4439421 1 8.70
CHEMBL4449563 1 7.55
CHEMBL4469739 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463644 IC50 = 2.0 nM 8.70
CHEMBL4439421 IC50 = 2.0 nM 8.70
CHEMBL4449563 IC50 = 28.0 nM 7.55
CHEMBL4469739 IC50 = 28.0 nM 7.55