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Assay Detail

CHEMBL3100299

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

Binding
Competitive inhibition of PGPH-like activity of human 20S proteasome beta 1 subunit assessed as hydrolysis of Z-LLE-AMC fluorogenic substrate Lineweaver-Burk plot analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proteasome component C5 (CHEMBL4208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
Hasegawa M, Yasuda Y, Tanaka M, Nakata K, Umeda E, Wang Y, Watanabe C, Uetake S, Kunoh T, Shionyu M, Sasaki R, Shiina I, Mizukami T.
Eur J Med Chem (2014) 71 : 290 -305
PubMed 24321833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.21 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099618 1 6.47
CHEMBL3099624 1 6.17
CHEMBL3099621 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099618 Ki = 340.0 nM 6.47
CHEMBL3099624 Ki = 670.0 nM 6.17
CHEMBL3099621 Ki = 1020.0 nM 5.99