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Assay Detail

CHEMBL5737620

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

Binding
High Throughput Screening (HTS) Assa: A high throughput screening (HTS) assay and together with NCATS screened over 350,000 compounds in attempt to identify novel GLS inhibitor structures.
27
Total Activities
8
Compounds Tested
3
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

Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.85 7.10
kon 9 - -
k_off 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814265 3 7.10
CHEMBL5880857 3 7.00
CHEMBL5896863 3 7.00
CHEMBL2178396 3 5.72
CHEMBL2178393 3 5.57
CHEMBL2177757 6 5.48
CHEMBL2177744 3 5.34
CHEMBL2177758 3 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814265 IC50 = 80.0 nM 7.10
CHEMBL5896863 IC50 = 100.0 nM 7.00
CHEMBL5880857 IC50 = 100.0 nM 7.00
CHEMBL2178396 IC50 = 1900.0 nM 5.72
CHEMBL2178393 IC50 = 2700.0 nM 5.57
CHEMBL2177757 IC50 = 3300.0 nM 5.48
CHEMBL2177757 IC50 = 3300.0 nM 5.48
CHEMBL2177744 IC50 = 4600.0 nM 5.34
CHEMBL2177758 IC50 = 100000.0 nM 4.00
CHEMBL2177757 kon = - -
CHEMBL2177757 k_off = - s-1 -
CHEMBL2178393 kon = - -
CHEMBL2178393 k_off = - s-1 -
CHEMBL2177758 kon = - -
CHEMBL2177758 k_off = - s-1 -
CHEMBL2178396 kon = - -
CHEMBL2178396 k_off = - s-1 -
CHEMBL2177744 k_off = - s-1 -
CHEMBL2177757 kon = - -
CHEMBL5896863 k_off = - s-1 -
CHEMBL5896863 kon = - -
CHEMBL5880857 k_off = - s-1 -
CHEMBL5880857 kon = - -
CHEMBL3814265 k_off = - s-1 -
CHEMBL3814265 kon = - -
CHEMBL2177744 kon = - -
CHEMBL2177757 k_off = - s-1 -