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Assay Detail

CHEMBL4704271

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

Binding
Inhibition of human 20S immunoproteasome beta 5 chymotrypsin-like activity in human KARPAS-1106P cells incubated for 2 hrs by proteasome-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type KARPAS-1106P
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteasome subunit beta type-8 (CHEMBL5620)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Zhan W,Singh PK,Ban Y,Qing X,Ah Kioon MD,Fan H,Zhao Q,Wang R,Sukenick G,Salmon J,Warren JD,Ma X,Barrat FJ,Nathan CF,Lin G
J Med Chem (2020) 63 : 13103 -13123
PubMed 33095579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.40 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4759896 1 7.82
CHEMBL4763116 1 7.62
CHEMBL4741140 1 7.55
CHEMBL4758484 1 7.41
CHEMBL4796570 1 7.28
CHEMBL4799140 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4759896 IC50 = 15.0 nM 7.82
CHEMBL4763116 IC50 = 24.0 nM 7.62
CHEMBL4741140 IC50 = 28.0 nM 7.55
CHEMBL4758484 IC50 = 39.0 nM 7.41
CHEMBL4796570 IC50 = 53.0 nM 7.28
CHEMBL4799140 IC50 = 197.0 nM 6.71