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Assay Detail

CHEMBL5326702

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

Binding
Inhibition of USP28 (149 to 703 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using Ub-AMC as substrate by fluorescence based analysis
24
Total Activities
24
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

Ubiquitin carboxyl-terminal hydrolase 28 (CHEMBL2157853)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.
Zhou D, Xu Z, Huang Y, Wang H, Zhu X, Zhang W, Song W, Gao T, Liu T, Wang M, Shi L, Zhang N, Xiong B.
Eur J Med Chem (2023) 254 : 115369 -115369
PubMed 37075624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.99 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5401467 1 7.40
CHEMBL5431014 1 7.00
CHEMBL5398929 1 6.96
CHEMBL5402874 1 6.82
CHEMBL5418668 1 6.52
CHEMBL5400775 1 6.44
CHEMBL5410351 1 5.95
CHEMBL5399446 1 5.67
CHEMBL5406507 1 5.55
CHEMBL5419136 1 5.53
CHEMBL5410474 1 5.37
CHEMBL473417 VISMODEGIB 4.0 1 5.32
CHEMBL5426174 1 5.25
CHEMBL5399208 1 5.07
CHEMBL5439629 1 4.96
CHEMBL5428159 1 -
CHEMBL5409128 1 -
CHEMBL5411940 1 -
CHEMBL5395831 1 -
CHEMBL5433505 1 -
CHEMBL5430206 1 -
CHEMBL5435891 1 -
CHEMBL5398668 1 -
CHEMBL5398084 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5401467 IC50 = 40.0 nM 7.40
CHEMBL5431014 IC50 = 100.0 nM 7.00
CHEMBL5398929 IC50 = 110.0 nM 6.96
CHEMBL5402874 IC50 = 150.0 nM 6.82
CHEMBL5418668 IC50 = 300.0 nM 6.52
CHEMBL5400775 IC50 = 360.0 nM 6.44
CHEMBL5410351 IC50 = 1130.0 nM 5.95
CHEMBL5399446 IC50 = 2130.0 nM 5.67
CHEMBL5406507 IC50 = 2820.0 nM 5.55
CHEMBL5419136 IC50 = 2940.0 nM 5.53
CHEMBL5410474 IC50 = 4240.0 nM 5.37
CHEMBL473417 VISMODEGIB IC50 = 4810.0 nM 5.32
CHEMBL5426174 IC50 = 5680.0 nM 5.25
CHEMBL5399208 IC50 = 8580.0 nM 5.07
CHEMBL5439629 IC50 = 11000.0 nM 4.96
CHEMBL5428159 IC50 - -
CHEMBL5409128 IC50 - -
CHEMBL5411940 IC50 - -
CHEMBL5395831 IC50 - -
CHEMBL5433505 IC50 - -
CHEMBL5430206 IC50 - -
CHEMBL5435891 IC50 - -
CHEMBL5398668 IC50 - -
CHEMBL5398084 IC50 - -