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Assay Detail

CHEMBL4704589

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

Binding
Covalent inhibition of human Notum (S81-T451 residues) C330S mutant expressed in HEK293S cells using OPTS substrate incubated for 40 mins by fluorescence based assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit.
Mahy W,Willis NJ,Zhao Y,Woodward HL,Svensson F,Sipthorp J,Vecchia L,Ruza RR,Hillier J,Kjær S,Frew S,Monaghan A,Bictash M,Salinas PC,Whiting P,Vincent JP,Jones EY,Fish PV
J Med Chem (2020) 63 : 12942 -12956
PubMed 33124429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.77 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174188 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174188 IC50 = 170.0 nM 6.77