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Assay Detail

CHEMBL4610865

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

Binding
Inhibition of SMO-mediated Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in sonic hedgehog-induced osteoblast differentiation by measuring alkaline phosphatase activity incubated for 72 hrs
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type C3H 10T1/2
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 27 8.24 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644674 1 9.10
CHEMBL4639432 1 9.05
CHEMBL4643226 1 9.00
CHEMBL4632769 1 9.00
CHEMBL4648026 1 8.96
CHEMBL4637249 1 8.77
CHEMBL4644175 1 8.64
CHEMBL4637222 1 8.59
CHEMBL4640840 1 8.54
CHEMBL4636369 1 8.54
CHEMBL4637218 1 8.51
CHEMBL4647379 1 8.51
CHEMBL473417 VISMODEGIB 4.0 1 8.33
CHEMBL4641050 1 8.17
CHEMBL2059867 1 8.17
CHEMBL4642917 1 8.12
CHEMBL2059865 1 7.89
CHEMBL4638476 1 7.89
CHEMBL4636326 1 7.77
CHEMBL2059861 1 7.75
CHEMBL2059868 1 7.68
CHEMBL4636352 1 7.64
CHEMBL2059869 1 7.57
CHEMBL4637915 1 7.52
CHEMBL2059860 1 7.41
CHEMBL2059866 1 7.05
CHEMBL4646211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644674 EC50 = 0.8 nM 9.10
CHEMBL4639432 EC50 = 0.9 nM 9.05
CHEMBL4643226 EC50 = 1.0 nM 9.00
CHEMBL4632769 EC50 = 1.0 nM 9.00
CHEMBL4648026 EC50 = 1.1 nM 8.96
CHEMBL4637249 EC50 = 1.7 nM 8.77
CHEMBL4644175 EC50 = 2.3 nM 8.64
CHEMBL4637222 EC50 = 2.6 nM 8.59
CHEMBL4640840 EC50 = 2.9 nM 8.54
CHEMBL4636369 EC50 = 2.9 nM 8.54
CHEMBL4637218 EC50 = 3.1 nM 8.51
CHEMBL4647379 EC50 = 3.1 nM 8.51
CHEMBL473417 VISMODEGIB EC50 = 4.7 nM 8.33
CHEMBL4641050 EC50 = 6.8 nM 8.17
CHEMBL2059867 EC50 = 6.7 nM 8.17
CHEMBL4642917 EC50 = 7.5 nM 8.12
CHEMBL2059865 EC50 = 13.0 nM 7.89
CHEMBL4638476 EC50 = 13.0 nM 7.89
CHEMBL4636326 EC50 = 17.0 nM 7.77
CHEMBL2059861 EC50 = 18.0 nM 7.75
CHEMBL2059868 EC50 = 21.0 nM 7.68
CHEMBL4636352 EC50 = 23.0 nM 7.64
CHEMBL2059869 EC50 = 27.0 nM 7.57
CHEMBL4637915 EC50 = 30.0 nM 7.52
CHEMBL2059860 EC50 = 39.0 nM 7.41
CHEMBL2059866 EC50 = 89.0 nM 7.05
CHEMBL4646211 EC50 < 1.5 nM -