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Assay Detail

CHEMBL3388366

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

Binding
Inhibition of trypsin-like activity of human inducible 20S immunoproteasome incubated for 15 mins before fluorogenic substrate addition
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5 5.43 5.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3357584 1 5.76
CHEMBL3357585 1 5.76
CHEMBL3357582 1 5.61
CHEMBL3357583 1 5.45
CHEMBL2337849 1 4.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3357584 IC50 = 1750.0 nM 5.76
CHEMBL3357585 IC50 = 1730.0 nM 5.76
CHEMBL3357582 IC50 = 2430.0 nM 5.61
CHEMBL3357583 IC50 = 3530.0 nM 5.45
CHEMBL2337849 IC50 = 27700.0 nM 4.56