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Assay Detail

CHEMBL4403375

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

Binding
Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based 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

Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.
Xi J, Zhuang R, Kong L, He R, Zhu H, Zhang J.
Eur J Med Chem (2019) 182 : 111646 -111646
PubMed 31521028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.21 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270515 DELANZOMIB 2.0 1 8.52
CHEMBL2141296 IXAZOMIB 3.0 1 8.47
CHEMBL371405 MARIZOMIB 3.0 1 8.46
CHEMBL451887 CARFILZOMIB 4.0 1 8.22
CHEMBL325041 BORTEZOMIB 3.0 1 8.15
CHEMBL2103884 OPROZOMIB 2.0 1 7.44
CHEMBL4297468 ZETOMIPZOMIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270515 DELANZOMIB IC50 = 3.0 nM 8.52
CHEMBL2141296 IXAZOMIB IC50 = 3.4 nM 8.47
CHEMBL371405 MARIZOMIB IC50 = 3.5 nM 8.46
CHEMBL451887 CARFILZOMIB IC50 = 6.0 nM 8.22
CHEMBL325041 BORTEZOMIB IC50 = 7.0 nM 8.15
CHEMBL2103884 OPROZOMIB IC50 = 36.0 nM 7.44
CHEMBL4297468 ZETOMIPZOMIB IC50 = 0.688 nM -