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Assay Detail

CHEMBL1007986

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

Binding
Inhibition of PGPH catalytic activity of 20S proteasome in human erythrocytes
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

Affinity labeling of the proteasome by a belactosin A derived inhibitor.
Hasegawa M, Kinoshita K, Nishimura C, Matsumura U, Shionyu M, Ikeda S, Mizukami T.
Bioorg Med Chem Lett (2008) 18 : 5668 -5671
PubMed 18801655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.82 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64925 MG-132 1 6.92
CHEMBL498970 1 6.82
CHEMBL491637 1 5.43
CHEMBL490829 1 5.08
CHEMBL491636 BELACTOSIN A 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64925 MG-132 IC50 = 120.0 nM 6.92
CHEMBL498970 IC50 = 150.0 nM 6.82
CHEMBL491637 IC50 = 3700.0 nM 5.43
CHEMBL490829 IC50 = 8300.0 nM 5.08
CHEMBL491636 BELACTOSIN A IC50 = 14000.0 nM 4.85