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Assay Detail

CHEMBL4150563

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

Binding
Inhibition of rhodamine-tagged FP probe binding to NOTUM in human SW620 cells conditioned media pretreated for 30 mins followed by rhodamine-tagged FP probe addition and measured after 30 mins by SDS-PAGE fluorescence analysis
6
Total Activities
6
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

Palmitoleoyl-protein carboxylesterase NOTUM (CHEMBL3714531)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling.
Suciu RM, Cognetta AB, Potter ZE, Cravatt BF.
ACS Med Chem Lett (2018) 9 : 563 -568
PubMed 29937983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.04 7.89
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174188 1 7.89
CHEMBL4163486 1 6.70
CHEMBL4160119 1 6.54
CHEMBL4170569 1 -
CHEMBL4170762 1 -
CHEMBL4171791 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174188 IC50 = 13.0 nM 7.89
CHEMBL4163486 IC50 = 200.0 nM 6.70
CHEMBL4160119 IC50 = 290.0 nM 6.54
CHEMBL4170569 Inhibition - % -
CHEMBL4170762 IC50 > 10000.0 nM -
CHEMBL4171791 IC50 > 10000.0 nM -