Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2162705

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

Binding
Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.
Wang J, Mook RA, Lu J, Gooden DM, Ribeiro A, Guo A, Barak LS, Lyerly HK, Chen W.
Bioorg Med Chem (2012) 20 : 6751 -6757
PubMed 23063522 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.83 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105737 SONIDEGIB 4.0 1 8.22
CHEMBL254129 CYCLOPAMINE 1 7.90
CHEMBL473417 VISMODEGIB 4.0 1 7.79
CHEMBL2160208 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105737 SONIDEGIB Ki = 6.0 nM 8.22
CHEMBL254129 CYCLOPAMINE Ki = 12.7 nM 7.90
CHEMBL473417 VISMODEGIB Ki = 16.2 nM 7.79
CHEMBL2160208 Ki = 37.9 nM 7.42