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Assay Detail

CHEMBL4309422

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

Binding
Inhibition of human KGA (1 to 669 residues) preincubated for 20 mins using 7 mM glutamine as substrate
5
Total Activities
5
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

Glutaminase kidney isoform, mitochondrial (CHEMBL2146302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.
Zimmermann SC, Duvall B, Tsukamoto T.
J Med Chem (2018) 62 : 45 -59
PubMed 29969024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.09 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177757 1 6.72
CHEMBL4456690 1 6.41
CHEMBL3664893 1 6.34
CHEMBL3664892 1 5.97
CHEMBL4452869 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177757 IC50 = 190.0 nM 6.72
CHEMBL4456690 IC50 = 390.0 nM 6.41
CHEMBL3664893 IC50 = 460.0 nM 6.34
CHEMBL3664892 IC50 = 1060.0 nM 5.97
CHEMBL4452869 IC50 = 10200.0 nM 4.99