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Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of PI3Kdelta in IgM stimulated human Raji cells incubated for 10 mins by AlphaLISA assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
Assay data:4 Active, 1 Activity ≤ 1 µM, 4 Tested
Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 4 Tested
Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
Assay data:30 Active, 29 Activity ≤ 1 µM, 30 Tested
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
Assay data:26 Active, 16 Activity ≤ 1 µM, 30 Tested
Enzyme Assay from US Patent US8653092: "Tetrahydro-pyrido-pyrimidine derivatives"
Assay data:94 Active, 94 Activity ≤ 1 µM, 94 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Ex-vivo inhibition of PI3Kdelta in po dosed Lewis rat assessed as reduction in anti-IgM/IL4-induced AKT phosphorylation at ser473 residue in whole blood pretreated up to 24 hrs followed by anti-IgM/IL4 stimulation after 10 mins by flow cytometric analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Dose normalized Cmax in cynomolgus monkey at 0.3 mg/kg, po by RP-HPLC analysis
Dose normalized Cmax in Sprague-Dawley rat at 30 mg/kg, po by RP-HPLC analysis
Dose normalized Cmax in Sprague-Dawley rat at 3 mg/kg, po by RP-HPLC analysis
Inhibition of DNA-PK (unknown origin) using peptide substrate assessed as reduction in incorporation of radioactive 33p into substrate by liquid scintillation counting method
Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA
Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA
Inhibition of PI3Kdelta in mouse spleen cells assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation by beta counting based mixed lymphocyte reaction assay
Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA
Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA
Inhibition of PI3Kdelta in anti-CD3 stimulated human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation pretreated for 1 hr followed by anti-CD3 addition measured last 16 hrs of 56 hrs incubation by beta counting method
Inhibition of PI3Kdelta in human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation measured last 16 hrs of 4 days incubation by beta counting based mixed lymphocyte reaction assay
Inhibition of PI3Kdelta in 50% rat blood assessed as reduction in anti-IgM stimulated AKT phosphorylation at ser473 residue pretreated for 1.5 hr followed by anti-IgM stimulation after 10 mins by flow cytometric analysis
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