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Assay Detail

CHEMBL4610909

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

Binding
Displacement of BODIPY-labeled cyclopamine from mouse SMO transfected in human HeLa cells by competition binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein smoothened (CHEMBL6080)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Yang B, Hird AW, Bodnarchuk MS, Zheng X, Dakin L, Su Q, Daly K, Godin R, Hattersley MM, Brassil P, Redmond S, John Russell D, Janetka JW.
Bioorg Med Chem (2020) 28 : 115227 -115227
PubMed 31862310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.23 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473417 VISMODEGIB 4.0 1 8.70
CHEMBL2059865 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473417 VISMODEGIB EC50 = 2.0 nM 8.70
CHEMBL2059865 EC50 = 18.0 nM 7.75