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Assay Detail

CHEMBL4418451

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

Binding
Inhibition of TEV-cleavable hexa-histidine tagged USP28 (1 to 1077 residues) (unknown origin) using ubiquitin-rhodamine 110 as substrate preincubated for 30 mins followed by substrate addition and measured after 20 mins by fluorescence based assay
21
Total Activities
21
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

Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.33 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4585832 1 6.70
CHEMBL4459980 1 6.70
CHEMBL4587318 1 6.70
CHEMBL4462420 1 6.70
CHEMBL4160957 1 6.70
CHEMBL4166283 1 6.70
CHEMBL4451295 1 6.70
CHEMBL4584152 1 6.70
CHEMBL4443504 1 6.70
CHEMBL4162425 1 6.70
CHEMBL4440956 1 5.70
CHEMBL4533281 1 5.70
CHEMBL4176483 1 5.70
CHEMBL4571015 1 5.70
CHEMBL4452295 1 5.70
CHEMBL4566674 1 5.70
CHEMBL4300392 1 -
CHEMBL4444579 1 -
CHEMBL4169696 1 -
CHEMBL4448281 1 -
CHEMBL4173102 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4585832 IC50 = 200.0 nM 6.70
CHEMBL4459980 IC50 = 200.0 nM 6.70
CHEMBL4587318 IC50 = 200.0 nM 6.70
CHEMBL4462420 IC50 = 200.0 nM 6.70
CHEMBL4160957 IC50 = 200.0 nM 6.70
CHEMBL4166283 IC50 = 200.0 nM 6.70
CHEMBL4451295 IC50 = 200.0 nM 6.70
CHEMBL4584152 IC50 = 200.0 nM 6.70
CHEMBL4443504 IC50 = 200.0 nM 6.70
CHEMBL4162425 IC50 = 200.0 nM 6.70
CHEMBL4440956 IC50 = 2000.0 nM 5.70
CHEMBL4533281 IC50 = 2000.0 nM 5.70
CHEMBL4176483 IC50 = 2000.0 nM 5.70
CHEMBL4571015 IC50 = 2000.0 nM 5.70
CHEMBL4452295 IC50 = 2000.0 nM 5.70
CHEMBL4566674 IC50 = 2000.0 nM 5.70
CHEMBL4300392 IC50 < 200.0 nM -
CHEMBL4444579 IC50 < 200.0 nM -
CHEMBL4169696 IC50 < 200.0 nM -
CHEMBL4448281 IC50 < 200.0 nM -
CHEMBL4173102 IC50 < 200.0 nM -