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Antagonist activity at SMO D473H mutant (unknown origin) expressed in mouse TM3 cells coexpressing Gli-luc reporter gene assessed as inhibition of Hh-Ag1.5 induced Gli luciferase activity incubated for 48 hrs by luminescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at SMO receptor (unknown origin)
Inhibition of SMO in mouse 3T3/HH FlashII-7 cells at 100 nM incubated for 36 hrs in presence of SHH by Gli-luciferase reporter assay
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of SMO in mouse 3T3/HH FlashII-7 cells incubated for 36 hrs in presence of SHH by Gli-luciferase reporter assay
Assay data:8 Active, 9 Activity ≤ 1 µM, 13 Tested
Inhibition of endogenous mouse Smo overexpressed in mouse C3H 10T1/2 cells cotransfected with Gli reporter gene assessed as Gli luciferase activity by dual luciferase assay
Inhibition of endogenous human Smo overexpressed in mouse C3H 10T1/2 cells cotransfected with Gli reporter gene assessed as Gli luciferase activity by dual luciferase assay
Inhibition of Smo D473H mutant (unknown origin) expressed in mouse C3H 10T1/2 cells cotransfected with Gli reporter gene assessed as Gli luciferase activity by dual luciferase assay
Inhibition of wild type Smo (unknown origin) expressed in mouse C3H 10T1/2 cells cotransfected with Gli reporter gene assessed as Gli luciferase activity by dual luciferase assay
Binding affinity to human SMO (181 to 787 residues) expressed in human HEK293 cells assessed as radioactivity incubated for 2 hrs in presence of H3-labeled smo antagonist by ligand-displacement assay
Inhibition of Smo D473H mutant (unknown origin) expressed in mouse NIH3T3 cells cotransfected with Gli luciferase reporter gene assessed as Gli luciferase activity incubated for 48 hrs by Bright-Glo reagent based luciferase assay
Antagonist activity at resistant Smo D473H mutant (unknown origin) expressed in mouse C3H 10T1/2 cells cotransfected with Gli reporter gene assessed as Gli luciferase activity incubated for 24 hrs by dual luciferase assay
Antagonist activity at resistant Smo D473H mutant (unknown origin) in presence of GDC0449
Radioligand Competition Binding Assay from US Patent US9056865: "Pyridine-2-derivatives as smoothened receptor modulators"
Assay data:149 Active, 149 Activity ≤ 1 µM, 149 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Antagonist activity at SMO in mouse NIH3T3 cells preincubated for 2 hrs followed by ShhN stimulation and measured after 24 hrs in presence of GDC0449 by Bright-Glo luciferase assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at SMO in mouse NIH3T3 cells preincubated for 2 hrs followed by SAG stimulation and measured after 24 hrs in presence of GDC0449 by Bright-Glo luciferase assay
Antagonist activity at SMO in mouse NIH3T3 cells preincubated for 2 hrs followed by SAG stimulation and measured after 24 hrs in presence of GDC0449 by Bright-Glo luciferase assay
Assay data:1 Tested
Antagonist activity at SMO in mouse NIH3T3 cells preincubated for 2 hrs followed by SAG stimulation and measured after 24 hrs by Bright-Glo luciferase assay
Assay data:10 Active, 9 Activity ≤ 1 µM, 12 Tested
Agonist activity at SMO in mouse NIH3T3 cells incubated for 2 hrs by Bright-Glo luciferase assay
Assay data:12 Active, 12 Activity ≤ 1 µM, 24 Tested
Agonist activity at SMO in mouse NIH3T3 cells assessed as fluorescent intensity of ciliary SMO incubated for 12 hrs by fluorescence method
Assay data:7 Active, 7 Tested
Agonist activity at SMO in mouse NIH3T3 cells assessed as induction of SMO accumulation in primary cilia incubated for 12 hrs by fluorescence method
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