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Assay Detail

CHEMBL4197842

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

Binding
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells assessed as suppression of Wnt signaling after 48 hrs by Super-top flash reporter gene assay
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255164)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor.
Ma H, Chen Q, Zhu F, Zheng J, Li J, Zhang H, Chen S, Xing H, Luo L, Zheng LT, He S, Zhang X.
Eur J Med Chem (2018) 149 : 110 -121
PubMed 29499483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.76 9.14
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215992 1 9.14
CHEMBL3188386 WNT-974 2.0 1 9.05
CHEMBL4215124 1 8.72
CHEMBL3923788 1 8.68
CHEMBL3910011 1 8.19
CHEMBL473417 VISMODEGIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215992 IC50 = 0.72 nM 9.14
CHEMBL3188386 WNT-974 IC50 = 0.9 nM 9.05
CHEMBL4215124 IC50 = 1.9 nM 8.72
CHEMBL3923788 IC50 = 2.1 nM 8.68
CHEMBL3910011 IC50 = 6.5 nM 8.19
CHEMBL473417 VISMODEGIB Inhibition - % -