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Assay Detail

CHEMBL4772834

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

Binding
Inhibition of recombinant human SNEP2 (365 to 589 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis
53
Total Activities
53
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 2 (CHEMBL2176776)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzothiophene-2-carboxamide derivatives as SENPs inhibitors with selectivity within SENPs family.
Wang Z,Liu Y,Zhang J,Ullah S,Kang N,Zhao Y,Zhou H
Eur J Med Chem (2020) 204 : 112553 -112553
PubMed 32717481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 5.12 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4791433 1 6.25
CHEMBL4776158 1 6.16
CHEMBL4792569 1 5.92
CHEMBL4780770 1 5.85
CHEMBL4780586 1 5.80
CHEMBL4796113 1 5.66
CHEMBL4778045 1 5.64
CHEMBL4783695 1 5.62
CHEMBL4793952 1 5.60
CHEMBL4791044 1 5.46
CHEMBL4796293 1 5.46
CHEMBL4789655 1 5.41
CHEMBL4791142 1 5.33
CHEMBL4778402 1 5.32
CHEMBL4785749 1 5.31
CHEMBL4792795 1 5.30
CHEMBL4785280 1 5.29
CHEMBL4800446 1 5.27
CHEMBL4789800 1 5.23
CHEMBL4780660 1 5.23
CHEMBL4790106 1 5.21
CHEMBL4786762 1 5.19
CHEMBL4780417 1 5.17
CHEMBL4783089 1 5.16
CHEMBL4780306 1 5.13
CHEMBL4784778 1 5.13
CHEMBL4778786 1 5.11
CHEMBL4798900 1 5.10
CHEMBL4788149 1 5.09
CHEMBL4792661 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4791433 IC50 = 560.0 nM 6.25
CHEMBL4776158 IC50 = 690.0 nM 6.16
CHEMBL4792569 IC50 = 1200.0 nM 5.92
CHEMBL4780770 IC50 = 1400.0 nM 5.85
CHEMBL4780586 IC50 = 1600.0 nM 5.80
CHEMBL4796113 IC50 = 2200.0 nM 5.66
CHEMBL4778045 IC50 = 2300.0 nM 5.64
CHEMBL4783695 IC50 = 2400.0 nM 5.62
CHEMBL4793952 IC50 = 2500.0 nM 5.60
CHEMBL4791044 IC50 = 3500.0 nM 5.46
CHEMBL4796293 IC50 = 3500.0 nM 5.46
CHEMBL4789655 IC50 = 3900.0 nM 5.41
CHEMBL4791142 IC50 = 4700.0 nM 5.33
CHEMBL4778402 IC50 = 4800.0 nM 5.32
CHEMBL4785749 IC50 = 4900.0 nM 5.31
CHEMBL4792795 IC50 = 5000.0 nM 5.30
CHEMBL4785280 IC50 = 5100.0 nM 5.29
CHEMBL4800446 IC50 = 5400.0 nM 5.27
CHEMBL4789800 IC50 = 5900.0 nM 5.23
CHEMBL4780660 IC50 = 5900.0 nM 5.23
CHEMBL4790106 IC50 = 6200.0 nM 5.21
CHEMBL4786762 IC50 = 6400.0 nM 5.19
CHEMBL4780417 IC50 = 6700.0 nM 5.17
CHEMBL4783089 IC50 = 6900.0 nM 5.16
CHEMBL4784778 IC50 = 7400.0 nM 5.13
CHEMBL4780306 IC50 = 7400.0 nM 5.13
CHEMBL4778786 IC50 = 7700.0 nM 5.11
CHEMBL4798900 IC50 = 7900.0 nM 5.10
CHEMBL4788149 IC50 = 8100.0 nM 5.09
CHEMBL4792661 IC50 = 8200.0 nM 5.09
CHEMBL4778697 IC50 = 8600.0 nM 5.07
CHEMBL4789067 IC50 = 9300.0 nM 5.03
CHEMBL4788955 IC50 = 9300.0 nM 5.03
CHEMBL4782207 IC50 = 10700.0 nM 4.97
CHEMBL4787562 IC50 = 11000.0 nM 4.96
CHEMBL4792715 IC50 = 11500.0 nM 4.94
CHEMBL4782296 IC50 = 11600.0 nM 4.94
CHEMBL4789330 IC50 = 11400.0 nM 4.94
CHEMBL4776955 IC50 = 12200.0 nM 4.91
CHEMBL4783015 IC50 = 13900.0 nM 4.86
CHEMBL4793772 IC50 = 15800.0 nM 4.80
CHEMBL4799293 IC50 = 16800.0 nM 4.78
CHEMBL4787683 IC50 = 17100.0 nM 4.77
CHEMBL4786976 IC50 = 20700.0 nM 4.68
CHEMBL4790058 IC50 = 21900.0 nM 4.66
CHEMBL4793738 IC50 = 22400.0 nM 4.65
CHEMBL4787085 IC50 = 24300.0 nM 4.61
CHEMBL4798491 IC50 = 26200.0 nM 4.58
CHEMBL3961988 IC50 = 30000.0 nM 4.52
CHEMBL4776323 IC50 = 34200.0 nM 4.47