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Kinase Assay from Article 10.1111/j.1747-0285.2007.00615.x: "SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity."
Assay data:9 Active, 5 Activity ≤ 1 µM, 9 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
In vivo inhibition of SRC phosphorylation in PBMC derived from human PC3 cells bearing mouse model assessed as plasma compound concentration required to inhibit 50 % phosphorylation
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In vivo inhibition of SRC phosphorylation in PBMC derived from human PC3 cells bearing mouse model at 50 mg/kg
Assay data:1 Tested
SummaryRelated BioAssays by Target
In vivo inhibition of SRC phosphorylation in PBMC derived from human PC3 cells bearing mouse model at 5 mg/kg
Inhibition of Src autophosphorylation in mouse GL261 cells
Inhibition of SRC in transformed mouse NIH3T3 cells by SDS-PAGE based immunoblot assay
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of LPS-induced SRC phosphorylation in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation for 30 mins by Western blot method
Inhibition of Src signaling pathway in mouse BV2 cells assessed as suppression of LPS-induced NO release at 0.1 to 100 uM preincubated for 1 hr followed by LPS addition measured after 24 hrs relative to control by Griess assay
Assay data:3 Active, 6 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of Src signaling pathway in mouse BV2 cells assessed as suppression of LPS-induced NO release at 0.01 M preincubated for 1 hr followed by LPS addition measured after 24 hrs relative to control by Griess assay
Assay data:9 Tested
Inhibition of Src in mouse BV2 cells assessed as suppression of LPS-induced NO release preincubated for 1 hr followed by LPS addition measured after 24 hrs by Griess assay
Assay data:5 Active, 36 Tested
Genome-wide siRNA screen of genes regulating the Lipopolysaccharide-induced NF-kappaB and TNF-alpha responses in mouse macrophages_Primary screen NFkB readout
Assay data:762 Active, 16821 Tested
SummaryRelated BioAssays by Same Project
Genome-wide siRNA screen of genes regulating the Lipopolysaccharide-induced NF-kappaB and TNF-alpha responses in mouse macrophages_Primary screen TNF readout
Assay data:1106 Active, 16821 Tested
A screen to identify the genes that modify the response of osteosarcoma to doxorubicin in mouse - Primary Screen
Assay data:788 Active, 16789 Tested
SummaryPubMed Citation
Inhibition of c-SRC phosphorylation at Y416 in mouse 32D cells expressing BCR/ABL fusion protein p210 at 1 uM by Western blotting analysis
Assay data:4 Active, 4 Tested
Inhibition of Tel-fused SRC in mouse BA/F3 cells
Assay data:5 Active, 6 Tested
Inhibition of EGF-srimulated SRC phosphorylation in mouse NIH/3T3 cells overexpressing human EGFR at 40 uM after 15 to 60 mins by immunoblotting
Assay data:2 Tested
Inhibition of constitutive SRC phosphorylation in v-Src transformed mouse NIH/3T3 cells at 40 or 50 uM after 12 to 48 hrs by immunoblotting
Assay data:4 Tested
Increase in Src kinase phosphorylation in mouse MC3T3-E1 cells at 1 uM
Assay data:1 Active, 1 Tested
Reversal of increase in Src kinase phosphorylation in mouse MC3T3-E1 cells transfected with dominant-negative mutant Src expression vector at 1 uM
Reversal of increase in Src kinase phosphorylation in mouse MC3T3-E1 cells at 1 uM in presence of PP2
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