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Assay Detail

CHEMBL2060771

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

Binding
Inhibition of Smo expressed in mouse C3H10T1/2 cells assessed as reduction in alkaline phosphatase level after 72 hrs by spectrophotometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C3H 10T1/2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
Yang B, Hird AW, Russell DJ, Fauber BP, Dakin LA, Zheng X, Su Q, Godin R, Brassil P, Devereaux E, Janetka JW.
Bioorg Med Chem Lett (2012) 22 : 4907 -4911
PubMed 22704236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.66 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2059867 1 8.15
CHEMBL2057336 1 8.10
CHEMBL2059870 1 8.10
CHEMBL2059862 1 7.96
CHEMBL2059865 1 7.89
CHEMBL2059864 1 7.82
CHEMBL2059875 1 7.77
CHEMBL2059861 1 7.75
CHEMBL2059868 1 7.68
CHEMBL2059863 1 7.66
CHEMBL2059869 1 7.57
CHEMBL2059873 1 7.55
CHEMBL2059871 1 7.54
CHEMBL2059859 1 7.52
CHEMBL2059860 1 7.41
CHEMBL2059876 1 7.40
CHEMBL2059866 1 7.05
CHEMBL2057337 1 6.94
CHEMBL2059874 1 -
CHEMBL2059872 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2059867 EC50 = 7.0 nM 8.15
CHEMBL2057336 EC50 = 8.0 nM 8.10
CHEMBL2059870 EC50 = 8.0 nM 8.10
CHEMBL2059862 EC50 = 11.0 nM 7.96
CHEMBL2059865 EC50 = 13.0 nM 7.89
CHEMBL2059864 EC50 = 15.0 nM 7.82
CHEMBL2059875 EC50 = 17.0 nM 7.77
CHEMBL2059861 EC50 = 18.0 nM 7.75
CHEMBL2059868 EC50 = 21.0 nM 7.68
CHEMBL2059863 EC50 = 22.0 nM 7.66
CHEMBL2059869 EC50 = 27.0 nM 7.57
CHEMBL2059873 EC50 = 28.0 nM 7.55
CHEMBL2059871 EC50 = 29.0 nM 7.54
CHEMBL2059859 EC50 = 30.0 nM 7.52
CHEMBL2059860 EC50 = 39.2 nM 7.41
CHEMBL2059876 EC50 = 40.0 nM 7.40
CHEMBL2059866 EC50 = 89.0 nM 7.05
CHEMBL2057337 EC50 = 115.0 nM 6.94
CHEMBL2059874 EC50 - -
CHEMBL2059872 EC50 > 145.0 nM -