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

CHEMBL2033036

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

Binding
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.
Solinas A, Faure H, Roudaut H, Traiffort E, Schoenfelder A, Mann A, Manetti F, Taddei M, Ruat M.
J Med Chem (2012) 55 : 1559 -1571
PubMed 22268551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.42 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2031290 1 8.30
CHEMBL473417 VISMODEGIB 4.0 1 8.15
CHEMBL2031277 1 7.62
CHEMBL2031268 1 7.20
CHEMBL254129 CYCLOPAMINE 1 7.19
CHEMBL2031273 1 6.97
CHEMBL2031084 1 6.52
CHEMBL480889 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2031290 IC50 = 5.0 nM 8.30
CHEMBL473417 VISMODEGIB IC50 = 7.0 nM 8.15
CHEMBL2031277 IC50 = 24.0 nM 7.62
CHEMBL2031268 IC50 = 63.0 nM 7.20
CHEMBL254129 CYCLOPAMINE IC50 = 64.0 nM 7.19
CHEMBL2031273 IC50 = 107.0 nM 6.97
CHEMBL2031084 IC50 = 300.0 nM 6.52
CHEMBL480889 IC50 - -