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Assay Detail

CHEMBL3626166

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

Binding
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as reduction in Wnt ligand-driven LEF/TCF-dependent transcriptional activity
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Wnt3A
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors.
Dong Y, Li K, Xu Z, Ma H, Zheng J, Hu Z, He S, Wu Y, Sun Z, Luo L, Li J, Zhang H, Zhang X.
Bioorg Med Chem (2015) 23 : 6855 -6868
PubMed 26455655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.25 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623895 1 9.96
CHEMBL3623894 1 9.72
CHEMBL3623875 1 9.64
CHEMBL3623893 1 9.28
CHEMBL3623896 1 9.24
CHEMBL3623892 1 9.17
CHEMBL3623891 1 9.02
CHEMBL3623874 1 8.66
CHEMBL3623887 1 8.57
CHEMBL3623873 1 8.30
CHEMBL3623889 1 7.62
CHEMBL3623879 1 7.52
CHEMBL3623878 1 7.40
CHEMBL3623877 1 6.79
CHEMBL3623876 1 6.73
CHEMBL3623890 1 6.32
CHEMBL3623888 1 6.31
CHEMBL3623886 1 -
CHEMBL3623885 1 -
CHEMBL3623884 1 -
CHEMBL3623883 1 -
CHEMBL3623882 1 -
CHEMBL3623881 1 -
CHEMBL3623880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623895 IC50 = 0.11 nM 9.96
CHEMBL3623894 IC50 = 0.19 nM 9.72
CHEMBL3623875 IC50 = 0.23 nM 9.64
CHEMBL3623893 IC50 = 0.53 nM 9.28
CHEMBL3623896 IC50 = 0.57 nM 9.24
CHEMBL3623892 IC50 = 0.67 nM 9.17
CHEMBL3623891 IC50 = 0.96 nM 9.02
CHEMBL3623874 IC50 = 2.2 nM 8.66
CHEMBL3623887 IC50 = 2.7 nM 8.57
CHEMBL3623873 IC50 = 5.0 nM 8.30
CHEMBL3623889 IC50 = 24.0 nM 7.62
CHEMBL3623879 IC50 = 30.0 nM 7.52
CHEMBL3623878 IC50 = 40.0 nM 7.40
CHEMBL3623877 IC50 = 164.0 nM 6.79
CHEMBL3623876 IC50 = 188.0 nM 6.73
CHEMBL3623890 IC50 = 483.0 nM 6.32
CHEMBL3623888 IC50 = 485.0 nM 6.31
CHEMBL3623886 IC50 > 1000.0 nM -
CHEMBL3623885 IC50 > 1000.0 nM -
CHEMBL3623884 IC50 > 1000.0 nM -
CHEMBL3623883 IC50 > 1000.0 nM -
CHEMBL3623882 IC50 > 1000.0 nM -
CHEMBL3623881 IC50 > 1000.0 nM -
CHEMBL3623880 IC50 > 1000.0 nM -