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Assay Detail

CHEMBL5165026

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

Binding
Inhibition of GLS1 in mouse brain assessed as inhibition of glutamate production using glutamine as substrate incubated for 1 hr by coupled assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles.
Xu X, Chang X, Huang J, Zhang D, Wang M, Jing T, Zhuang Y, Kou J, Qiu Z, Wang J, Li Z, Bian J.
Eur J Med Chem (2022) 236 : 114337 -114337
PubMed 35428013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3639788 TELAGLENASTAT 2.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3639788 TELAGLENASTAT IC50 = 20.0 nM 7.70