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Assay Detail

CHEMBL4479671

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

Binding
Inhibition of recombinant human 6His-tagged SENP1 catalytic domain expressed in Escherichia coli preincubated for 15 mins followed by addition of SUMO1-AMC as substrate measured after 1 hr by fluorescence analysis
5
Total Activities
5
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

Sentrin-specific protease 1 (CHEMBL1909484)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity.
Yoshioka Y, Namiki D, Makiuchi M, Sugaya K, Onose J, Ashida H, Abe N.
Bioorg Med Chem Lett (2016) 26 : 4237 -4240
PubMed 27491710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.44 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4587307 1 5.82
CHEMBL2012938 VIALININ A 1 5.72
CHEMBL2012939 1 5.42
CHEMBL4593579 1 5.21
CHEMBL2013072 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587307 IC50 = 1520.0 nM 5.82
CHEMBL2012938 VIALININ A IC50 = 1890.0 nM 5.72
CHEMBL2012939 IC50 = 3760.0 nM 5.42
CHEMBL4593579 IC50 = 6100.0 nM 5.21
CHEMBL2013072 IC50 = 9730.0 nM 5.01