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Assay Detail

CHEMBL950132

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

Binding
Inhibition of trypsin-like activity of 20S proteasome
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Vinyl ester-based cyclic peptide proteasome inhibitors.
Baldisserotto A, Marastoni M, Fiorini S, Pretto L, Ferretti V, Gavioli R, Tomatis R.
Bioorg Med Chem Lett (2008) 18 : 1849 -1854
PubMed 18294845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.55 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404589 1 6.89
CHEMBL401549 1 6.87
CHEMBL402250 1 6.81
CHEMBL257878 1 6.76
CHEMBL207990 EPOXOMYCIN 1 6.55
CHEMBL250260 1 6.54
CHEMBL255202 1 6.41
CHEMBL406699 1 6.37
CHEMBL271417 1 6.35
CHEMBL64925 MG-132 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404589 IC50 = 129.0 nM 6.89
CHEMBL401549 IC50 = 134.0 nM 6.87
CHEMBL402250 IC50 = 155.0 nM 6.81
CHEMBL257878 IC50 = 175.0 nM 6.76
CHEMBL207990 EPOXOMYCIN IC50 = 284.0 nM 6.55
CHEMBL250260 IC50 = 286.0 nM 6.54
CHEMBL255202 IC50 = 389.0 nM 6.41
CHEMBL406699 IC50 = 424.0 nM 6.37
CHEMBL271417 IC50 = 447.0 nM 6.35
CHEMBL64925 MG-132 IC50 = 1077.0 nM 5.97