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Assay Detail

CHEMBL2162808

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

Binding
Inhibition of recombinant His-tagged SENP1 catalytic domain expressed in Escherichia coli BL21(DE3) using His-tagged deltaRanGAP-SUMO2 as substrate incubated for 10 mins prior to substrate addition measured after 45 mins by SDS-PAGE analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.
Chen Y, Wen D, Huang Z, Huang M, Luo Y, Liu B, Lu H, Wu Y, Peng Y, Zhang J.
Bioorg Med Chem Lett (2012) 22 : 6867 -6870
PubMed 23044371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.74 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159857 1 5.97
CHEMBL2159858 1 5.93
CHEMBL2159859 1 5.76
CHEMBL2159862 1 5.73
CHEMBL2159861 1 5.62
CHEMBL2159860 1 5.45
CHEMBL2159852 1 -
CHEMBL2159854 1 -
CHEMBL2159856 1 -
CHEMBL2159855 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159857 IC50 = 1080.0 nM 5.97
CHEMBL2159858 IC50 = 1175.0 nM 5.93
CHEMBL2159859 IC50 = 1735.0 nM 5.76
CHEMBL2159862 IC50 = 1856.0 nM 5.73
CHEMBL2159861 IC50 = 2385.0 nM 5.62
CHEMBL2159860 IC50 = 3542.0 nM 5.45
CHEMBL2159852 IC50 > 50000.0 nM -
CHEMBL2159854 IC50 > 50000.0 nM -
CHEMBL2159856 IC50 > 50000.0 nM -
CHEMBL2159855 IC50 > 50000.0 nM -