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Assay Detail

CHEMBL3705630

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

Binding
Enzyme Assay-Time Dependence: Compounds were assessed for their ability to inhibit the enzymatic activity of a recombinant form of Glutaminase 1 (GAC) using a biochemical assay that couples the production of glutamate (liberated by GAC) to glutamate dehydrogenase (GDH) and measuring the change in absorbance for the reduction of NAD+ to NADH.
330
Total Activities
326
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

Heterocyclic inhibitors of glutaminase
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 330 7.86 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3675017 1 8.70
CHEMBL3675018 1 8.70
CHEMBL3675020 1 8.70
CHEMBL3675057 1 8.70
CHEMBL3675059 1 8.70
CHEMBL3680041 1 8.70
CHEMBL3675079 1 8.52
CHEMBL3675055 1 8.52
CHEMBL3675081 1 8.52
CHEMBL3675099 1 8.52
CHEMBL3675100 1 8.52
CHEMBL3675141 2 8.52
CHEMBL3675140 1 8.52
CHEMBL3675150 1 8.52
CHEMBL3675153 1 8.52
CHEMBL3679964 1 8.52
CHEMBL3679978 1 8.52
CHEMBL3675067 1 8.52
CHEMBL3675058 1 8.52
CHEMBL3675054 1 8.52
CHEMBL3675043 1 8.52
CHEMBL3675041 1 8.52
CHEMBL3675040 1 8.52
CHEMBL3675038 1 8.52
CHEMBL3675036 1 8.52
CHEMBL3675029 1 8.52
CHEMBL3674970 1 8.52
CHEMBL3674968 1 8.52
CHEMBL3674980 1 8.40
CHEMBL3674981 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3675057 IC50 = 2.0 nM 8.70
CHEMBL3675059 IC50 = 2.0 nM 8.70
CHEMBL3675020 IC50 = 2.0 nM 8.70
CHEMBL3680041 IC50 = 2.0 nM 8.70
CHEMBL3675018 IC50 = 2.0 nM 8.70
CHEMBL3675017 IC50 = 2.0 nM 8.70
CHEMBL3675081 IC50 = 3.0 nM 8.52
CHEMBL3675029 IC50 = 3.0 nM 8.52
CHEMBL3675079 IC50 = 3.0 nM 8.52
CHEMBL3679964 IC50 = 3.0 nM 8.52
CHEMBL3674968 IC50 = 3.0 nM 8.52
CHEMBL3675036 IC50 = 3.0 nM 8.52
CHEMBL3674970 IC50 = 3.0 nM 8.52
CHEMBL3679978 IC50 = 3.0 nM 8.52
CHEMBL3675038 IC50 = 3.0 nM 8.52
CHEMBL3675040 IC50 = 3.0 nM 8.52
CHEMBL3675041 IC50 = 3.0 nM 8.52
CHEMBL3675153 IC50 = 3.0 nM 8.52
CHEMBL3675043 IC50 = 3.0 nM 8.52
CHEMBL3675140 IC50 = 3.0 nM 8.52
CHEMBL3675141 IC50 = 3.0 nM 8.52
CHEMBL3675058 IC50 = 3.0 nM 8.52
CHEMBL3675055 IC50 = 3.0 nM 8.52
CHEMBL3675054 IC50 = 3.0 nM 8.52
CHEMBL3675099 IC50 = 3.0 nM 8.52
CHEMBL3675100 IC50 = 3.0 nM 8.52
CHEMBL3675150 IC50 = 3.0 nM 8.52
CHEMBL3675067 IC50 = 3.0 nM 8.52
CHEMBL3675117 IC50 = 4.0 nM 8.40
CHEMBL3675121 IC50 = 4.0 nM 8.40
CHEMBL3679985 IC50 = 4.0 nM 8.40
CHEMBL3675120 IC50 = 4.0 nM 8.40
CHEMBL3675080 IC50 = 4.0 nM 8.40
CHEMBL3675068 IC50 = 4.0 nM 8.40
CHEMBL3679965 IC50 = 4.0 nM 8.40
CHEMBL3679971 IC50 = 4.0 nM 8.40
CHEMBL3674980 IC50 = 4.0 nM 8.40
CHEMBL3674981 IC50 = 4.0 nM 8.40
CHEMBL3675155 IC50 = 4.0 nM 8.40
CHEMBL3675154 IC50 = 4.0 nM 8.40
CHEMBL3675154 IC50 = 4.0 nM 8.40
CHEMBL3675069 IC50 = 4.0 nM 8.40
CHEMBL3675151 IC50 = 4.0 nM 8.40
CHEMBL3674983 IC50 = 4.0 nM 8.40
CHEMBL3675014 IC50 = 4.0 nM 8.40
CHEMBL3679966 IC50 = 4.0 nM 8.40
CHEMBL3675134 IC50 = 4.0 nM 8.40
CHEMBL3675142 IC50 = 4.0 nM 8.40
CHEMBL3679967 IC50 = 4.0 nM 8.40
CHEMBL3675167 IC50 = 4.0 nM 8.40