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Assay Detail

CHEMBL4309433

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Binding
Inhibition of mouse kidney glutaminase assessed as ammonia formation at 0.1 uM using glutamine as substrate by Nessler's reagent based assay relative to control
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutaminase kidney isoform, mitochondrial (CHEMBL4523110)
Type SINGLE PROTEIN
Organism Mus musculus

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 6.65 7.30
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462220 1 7.30
CHEMBL4537860 1 6.00
CHEMBL4577734 1 -
CHEMBL4452754 1 -
CHEMBL4540444 1 -
CHEMBL4441898 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462220 IC50 = 50.0 nM 7.30
CHEMBL4537860 IC50 = 1000.0 nM 6.00
CHEMBL4577734 IC50 < 50.0 nM -
CHEMBL4452754 IC50 < 50.0 nM -
CHEMBL4540444 IC50 < 25.0 nM -
CHEMBL4441898 Inhibition <= 25.0 % -