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Assay Detail

CHEMBL5151003

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

Binding
Inhibition of human Notum using OPTS substrate by fluorescence based assay
7
Total Activities
7
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

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

Publication

Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.
Bayle ED, Svensson F, Atkinson BN, Steadman D, Willis NJ, Woodward HL, Whiting P, Vincent JP, Fish PV.
J Med Chem (2021) 64 : 4289 -4311
PubMed 33783220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.64 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3760062 1 9.40
CHEMBL3774760 1 9.00
CHEMBL3774528 1 8.70
CHEMBL4174188 1 6.77
CHEMBL284521 1 4.43
CHEMBL45 MELATONIN 4.0 1 4.12
CHEMBL33103 ACETYLSEROTONIN 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3760062 IC50 = 0.4 nM 9.40
CHEMBL3774760 IC50 = 1.0 nM 9.00
CHEMBL3774528 IC50 = 2.0 nM 8.70
CHEMBL4174188 IC50 = 170.0 nM 6.77
CHEMBL284521 IC50 = 37200.0 nM 4.43
CHEMBL45 MELATONIN IC50 = 75400.0 nM 4.12
CHEMBL33103 ACETYLSEROTONIN IC50 = 93600.0 nM 4.03