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Assay Detail

CHEMBL832987

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Binding
Inhibition of trypsin like activity of the proteasome purified from lymphoblastoid cell lines (in vitro)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 2 — Organism
Curated By Expert

Target

Proteasome (CHEMBL612443)
Type SUBCELLULAR

Publication

Peptidyl vinyl ester derivatives: new class of selective inhibitors of proteasome trypsin-like activity.
Marastoni M, Baldisserotto A, Cellini S, Gavioli R, Tomatis R.
J Med Chem (2005) 48 : 5038 -5042
PubMed 16033282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.92 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188918 1 7.48
CHEMBL189919 1 7.39
CHEMBL188781 1 7.15
CHEMBL188385 1 6.96
CHEMBL189348 1 6.72
CHEMBL426081 1 6.68
CHEMBL365912 1 6.55
CHEMBL188437 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188918 IC50 = 33.0 nM 7.48
CHEMBL189919 IC50 = 41.0 nM 7.39
CHEMBL188781 IC50 = 71.0 nM 7.15
CHEMBL188385 IC50 = 110.0 nM 6.96
CHEMBL189348 IC50 = 190.0 nM 6.72
CHEMBL426081 IC50 = 210.0 nM 6.68
CHEMBL365912 IC50 = 280.0 nM 6.55
CHEMBL188437 IC50 = 380.0 nM 6.42