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Assay Detail

CHEMBL1062206

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

Binding
Inhibition of chymotrypsin trypsin-like activity of proteasome from human LCL after 30 mins by fluorimetry
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

N-terminal-prolonged vinyl ester-based peptides as selective proteasome beta1 subunit inhibitors.
Baldisserotto A, Destro F, Vertuani G, Marastoni M, Gavioli R, Tomatis R.
Bioorg Med Chem (2009) 17 : 5535 -5540
PubMed 19577931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.50 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64925 MG-132 1 8.70
CHEMBL207990 EPOXOMYCIN 1 8.30
CHEMBL559524 1 -
CHEMBL559132 1 -
CHEMBL538413 1 -
CHEMBL538414 1 -
CHEMBL559141 1 -
CHEMBL540478 1 -
CHEMBL553239 1 -
CHEMBL550238 1 -
CHEMBL552110 1 -
CHEMBL552111 1 -
CHEMBL560974 1 -
CHEMBL539909 1 -
CHEMBL556440 1 -
CHEMBL558733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64925 MG-132 IC50 = 2.0 nM 8.70
CHEMBL207990 EPOXOMYCIN IC50 = 5.0 nM 8.30
CHEMBL559524 IC50 > 10000.0 nM -
CHEMBL559132 IC50 > 10000.0 nM -
CHEMBL538413 IC50 > 10000.0 nM -
CHEMBL538414 IC50 > 10000.0 nM -
CHEMBL559141 IC50 > 10000.0 nM -
CHEMBL540478 IC50 > 10000.0 nM -
CHEMBL553239 IC50 > 10000.0 nM -
CHEMBL550238 IC50 > 10000.0 nM -
CHEMBL552110 IC50 > 10000.0 nM -
CHEMBL552111 IC50 > 10000.0 nM -
CHEMBL560974 IC50 > 10000.0 nM -
CHEMBL539909 IC50 > 10000.0 nM -
CHEMBL556440 IC50 > 10000.0 nM -
CHEMBL558733 IC50 > 10000.0 nM -