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Assay Detail

CHEMBL5625329

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

Binding
Inhibition of wild type IDH1 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as NADPH consumption using alpha-KG as substrate measured after 60 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

Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma.
Wang QX, Zhang PY, Li QQ, Tong ZJ, Wu JZ, Yu SP, Yu YC, Ding N, Leng XJ, Chang L, Xu JG, Sun SL, Yang Y, Li NG, Shi ZH.
Eur J Med Chem (2023) 257 : 115464 -115464
PubMed 37235998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.31 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439727 1 5.50
CHEMBL5632655 1 5.49
CHEMBL5631386 1 5.42
CHEMBL5633668 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439727 IC50 = 3200.0 nM 5.50
CHEMBL5632655 IC50 = 3230.0 nM 5.49
CHEMBL5631386 IC50 = 3800.0 nM 5.42
CHEMBL5633668 IC50 = 14400.0 nM 4.84