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Assay Detail

CHEMBL5371975

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Binding
Reversible binding affinity to IDH1 R132H mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant
1
Total Activities
1
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

Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor.
Liang Q, Wang B, Zou F, Guo G, Wang W, Wang W, Liu Q, Shen L, Hu C, Wang W, Wang A, Huang T, He Y, Xia R, Ge J, Liu J, Liu Q.
Eur J Med Chem (2023) 256 : 115411 -115411
PubMed 37209613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.43 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425749 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425749 Ki = 37.0 nM 7.43