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Assay Detail

CHEMBL3388367

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

Binding
Inhibition of chymotrypsin-like activity of proteasome in HEK293 cells incubated for 1 hr by proteasome Glo cell-based chemiluminescent assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 2 — Organism
Curated By Autocuration

Target

Proteasome (CHEMBL612443)
Type SUBCELLULAR

Publication

Noncovalent fluorescent probes of human immuno- and constitutive proteasomes.
Desvergne A, Cheng Y, Grosay-Gaudrel S, Maréchal X, Reboud-Ravaux M, Genin E, Vidal J.
J Med Chem (2014) 57 : 9211 -9217
PubMed 25333324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.88 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3357584 1 7.19
CHEMBL3357585 1 6.90
CHEMBL3357583 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3357584 IC50 = 65.0 nM 7.19
CHEMBL3357585 IC50 = 125.0 nM 6.90
CHEMBL3357583 IC50 = 289.0 nM 6.54