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Assay Detail

CHEMBL4369800

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

Binding
Inhibition of human recombinant GAC (72 to 598 residues) expressed in Escherichia coli BL21(DE3) after 10 mins by GluO-horseradish peroxidase coupled assay
2
Total Activities
2
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

Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity.
Chen Z, Li D, Xu N, Fang J, Yu Y, Hou W, Ruan H, Zhu P, Ma R, Lu S, Cao D, Wu R, Ni M, Zhang W, Su W, Ruan BH.
J Med Chem (2019) 62 : 589 -603
PubMed 30543285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.40 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177757 1 7.00
CHEMBL3664910 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177757 IC50 = 100.0 nM 7.00
CHEMBL3664910 IC50 = 1600.0 nM 5.80