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Assay Detail

CHEMBL4197876

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Functional
Inhibition of smo-mediated hedgehog signaling pathway in mouse NIH3T3 cells expressing GRE-Luc reporter gene assessed as inhibition of SAG-induced GRE-Luc reporter activity after 48 hrs by luminescence assay
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL6080)
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 4 6.68 8.22
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473417 VISMODEGIB 4.0 1 8.22
CHEMBL3972086 2 7.15
CHEMBL4215992 1 5.91
CHEMBL4215124 1 5.44
CHEMBL3188386 WNT-974 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473417 VISMODEGIB IC50 = 6.0 nM 8.22
CHEMBL3972086 IC50 = 71.0 nM 7.15
CHEMBL4215992 IC50 = 1223.0 nM 5.91
CHEMBL4215124 IC50 = 3661.0 nM 5.44
CHEMBL3188386 WNT-974 Inhibition - % -
CHEMBL3972086 Inhibition - % -