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Assay Detail

CHEMBL969912

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

Binding
In vivo inhibition of trypsin like 20S proteasome
5
Total Activities
5
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

C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors.
Baldisserotto A, Marastoni M, Lazzari I, Trapella C, Gavioli R, Tomatis R.
Eur J Med Chem (2008) 43 : 1403 -1411
PubMed 17996987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.48 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188918 1 7.30
CHEMBL447652 1 7.04
CHEMBL488905 1 6.64
CHEMBL448088 1 5.74
CHEMBL488718 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188918 IC50 = 50.0 nM 7.30
CHEMBL447652 IC50 = 92.0 nM 7.04
CHEMBL488905 IC50 = 231.0 nM 6.64
CHEMBL448088 IC50 = 1815.0 nM 5.74
CHEMBL488718 IC50 = 2179.0 nM 5.66