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Assay Detail

CHEMBL3095999

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

Binding
Inhibition of chymotrypsin like activity of human 20S proteasome after 1 hr by luminescence assay
7
Total Activities
7
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 Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(S)-4-Trimethylsilyl-3-butyn-2-ol as an auxiliary for stereocontrolled synthesis of salinosporamide analogs with modifications at positions C2 and C5.
Blasdel LK, Lee D, Sun B, Myers AG.
Bioorg Med Chem Lett (2013) 23 : 6905 -6910
PubMed 24269479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.03 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371405 MARIZOMIB 3.0 1 7.66
CHEMBL192046 1 7.64
CHEMBL3092609 1 7.55
CHEMBL3092608 1 7.30
CHEMBL3092611 1 6.48
CHEMBL3092612 1 6.30
CHEMBL3092610 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371405 MARIZOMIB IC50 = 22.0 nM 7.66
CHEMBL192046 IC50 = 23.0 nM 7.64
CHEMBL3092609 IC50 = 28.0 nM 7.55
CHEMBL3092608 IC50 = 50.0 nM 7.30
CHEMBL3092611 IC50 = 330.0 nM 6.48
CHEMBL3092612 IC50 = 500.0 nM 6.30
CHEMBL3092610 IC50 = 500.0 nM 6.30