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Assay Detail

CHEMBL4338312

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

Binding
Inhibition of IDH1 R132H mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 5 mins followed by substrate addition and measured every 1 min
10
Total Activities
10
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

Flavipesines A and B and Asperchalasines E-H: Cytochalasans and Merocytochalasans from Aspergillus flavipes.
Zhang X, Yang L, Wang W, Wu Z, Wang J, Sun W, Li XN, Chen C, Zhu H, Zhang Y.
J Nat Prod (2019) 82 : 2994 -3001
PubMed 31674782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.13 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180727 1 6.70
CHEMBL4590233 1 4.93
CHEMBL4562901 1 4.88
CHEMBL4575450 1 4.76
CHEMBL4580009 1 4.36
CHEMBL4542803 1 -
CHEMBL4439480 1 -
CHEMBL4439930 1 -
CHEMBL4442122 1 -
CHEMBL4557972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180727 IC50 = 200.0 nM 6.70
CHEMBL4590233 IC50 = 11660.0 nM 4.93
CHEMBL4562901 IC50 = 13310.0 nM 4.88
CHEMBL4575450 IC50 = 17310.0 nM 4.76
CHEMBL4580009 IC50 = 43580.0 nM 4.36
CHEMBL4542803 IC50 > 50000.0 nM -
CHEMBL4439480 IC50 > 50000.0 nM -
CHEMBL4439930 IC50 > 50000.0 nM -
CHEMBL4442122 IC50 > 50000.0 nM -
CHEMBL4557972 IC50 > 50000.0 nM -