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Assay Detail

CHEMBL4682121

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

Binding
Binding affinity to human 20S constitutive proteasome beta 5 subunit assessed as equilibrium constant using fluorogenic peptide Ac-WLA-AMC as substrate in presence of PA28alpha by fluorescence based microplate reader assay
1
Total Activities
1
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

Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
Xie SC,Gillett DL,Spillman NJ,Tsu C,Luth MR,Ottilie S,Duffy S,Gould AE,Hales P,Seager BA,Charron CL,Bruzzese F,Yang X,Zhao X,Huang SC,Hutton CA,Burrows JN,Winzeler EA,Avery VM,Dick LR,Tilley L
J Med Chem (2018) 61 : 10053 -10066
PubMed 30373366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.89 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749207 1 9.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749207 Ki = 0.13 nM 9.89