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Assay Detail

CHEMBL4196841

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

Binding
Inhibition of chymotrypsin-like activity of human 26S proteasome using Z-LLE-MCA as substrate measured for 1 hr in presence of ATPgammaS by fluorescence assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteasome Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.
Tanaka M, Zhu Y, Shionyu M, Ota N, Shibata N, Watanabe C, Mizusawa A, Sasaki R, Mizukami T, Shiina I, Hasegawa M.
Eur J Med Chem (2018) 146 : 636 -650
PubMed 29407987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.42 5.62
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4212401 1 5.62
CHEMBL4217338 1 5.22
CHEMBL3099618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4212401 IC50 = 2400.0 nM 5.62
CHEMBL4217338 IC50 = 6000.0 nM 5.22
CHEMBL3099618 Inhibition - % -