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Assay Detail

CHEMBL3762498

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

Binding
Inhibition of recombinant GST-fused SUMO E1 (unknown origin) using RanGAP1 as substrate after 2 hrs by immunoblot analysis
9
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

SUMO-activating enzyme subunit 1 (CHEMBL1615388)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of new SUMO activating enzyme 1 inhibitors using virtual screening and scaffold hopping.
Kumar A, Ito A, Hirohama M, Yoshida M, Zhang KY.
Bioorg Med Chem Lett (2016) 26 : 1218 -1223
PubMed 26810265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.48 4.87
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471230 1 4.87
CHEMBL3759613 1 4.86
CHEMBL3758249 1 4.52
CHEMBL3758566 2 4.48
CHEMBL3758383 1 4.14
CHEMBL3758250 2 4.03
CHEMBL3759177 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471230 IC50 = 13400.0 nM 4.87
CHEMBL3759613 IC50 = 13800.0 nM 4.86
CHEMBL3758249 IC50 = 30400.0 nM 4.52
CHEMBL3758566 IC50 = 33200.0 nM 4.48
CHEMBL3758383 IC50 = 73000.0 nM 4.14
CHEMBL3758250 IC50 = 92600.0 nM 4.03
CHEMBL3758250 Inhibition - % -
CHEMBL3758566 Inhibition - % -
CHEMBL3759177 IC50 > 100000.0 nM -