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Assay Detail

CHEMBL3413040

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Binding
Inhibition of hedgehog signaling in mouse C3H10T1/2 cells assessed as reduction in Gli1 mRNA level after 24 hrs by quantitative PCR analysis
30
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type C3H 10T1/2
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors.
DeBerardinis AM, Raccuia DS, Thompson EN, Maschinot CA, Kyle Hadden M.
Eur J Med Chem (2015) 93 : 156 -171
PubMed 25676864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 15 - -
IC50 15 5.90 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408016 2 6.50
CHEMBL3408015 2 6.40
CHEMBL2407295 2 6.13
CHEMBL3407996 2 6.10
CHEMBL3408158 2 6.01
CHEMBL3408162 2 6.00
CHEMBL3408014 2 6.00
CHEMBL3408163 2 5.92
CHEMBL3408013 2 5.92
CHEMBL3408161 2 5.82
CHEMBL3408012 2 5.75
CHEMBL3408165 2 5.62
CHEMBL3407998 2 5.58
CHEMBL3408007 2 5.41
CHEMBL1042 CHOLECALCIFEROL 4.0 2 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408016 IC50 = 320.0 nM 6.50
CHEMBL3408015 IC50 = 400.0 nM 6.40
CHEMBL2407295 IC50 = 740.0 nM 6.13
CHEMBL3407996 IC50 = 790.0 nM 6.10
CHEMBL3408158 IC50 = 980.0 nM 6.01
CHEMBL3408162 IC50 = 1000.0 nM 6.00
CHEMBL3408014 IC50 = 1000.0 nM 6.00
CHEMBL3408163 IC50 = 1200.0 nM 5.92
CHEMBL3408013 IC50 = 1200.0 nM 5.92
CHEMBL3408161 IC50 = 1500.0 nM 5.82
CHEMBL3408012 IC50 = 1800.0 nM 5.75
CHEMBL3408165 IC50 = 2400.0 nM 5.62
CHEMBL3407998 IC50 = 2600.0 nM 5.58
CHEMBL3408007 IC50 = 3900.0 nM 5.41
CHEMBL1042 CHOLECALCIFEROL IC50 = 4100.0 nM 5.39
CHEMBL3408163 Inhibition - % -
CHEMBL3408162 Inhibition - % -
CHEMBL3408161 Inhibition - % -
CHEMBL3408158 Inhibition - % -
CHEMBL3408016 Inhibition - % -
CHEMBL3408015 Inhibition - % -
CHEMBL3408014 Inhibition - % -
CHEMBL3408013 Inhibition - % -
CHEMBL3408012 Inhibition - % -
CHEMBL3408007 Inhibition - % -
CHEMBL3407998 Inhibition - % -
CHEMBL3407996 Inhibition - % -
CHEMBL2407295 Inhibition - % -
CHEMBL1042 CHOLECALCIFEROL Inhibition - % -
CHEMBL3408165 Inhibition - % -