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Assay Detail

CHEMBL4403374

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

Binding
Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assay
4
Total Activities
4
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 subunit beta type-10 (CHEMBL3317334)
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 4 7.53 9.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297468 ZETOMIPZOMIB 2.0 1 9.88
CHEMBL270515 DELANZOMIB 2.0 1 8.00
CHEMBL451887 CARFILZOMIB 4.0 1 6.21
CHEMBL325041 BORTEZOMIB 3.0 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297468 ZETOMIPZOMIB IC50 = 0.131 nM 9.88
CHEMBL270515 DELANZOMIB IC50 = 10.0 nM 8.00
CHEMBL451887 CARFILZOMIB IC50 = 620.0 nM 6.21
CHEMBL325041 BORTEZOMIB IC50 = 940.0 nM 6.03