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Antitumor activity against human KARPAS-422 cells xenografted in mouse at 40 mg/kg via oral gavage and mesured after 32 days by caliper method relative to control
Assay data:1 Tested
Summary
Synergistic growth inhibition against human KARPAS-422 cells assessed as reduction in H3K27me3 level by measuring synergistic score upto 10 uM measured after 4 days in presence of EI1
Synergistic growth inhibition against human KARPAS-422 cells assessed as reduction in cell proliferation by measuring synergistic score at upto 10 uM measured after 6 days in presence of EI1
Binding affinity to PRC2 complex of EZH2-EED-SUZ12 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryRelated BioAssays by Target
Stabilization of PRC2 complex of EZH2-EED-SUZ12 (unknown origin) assessed as thermal stability by measuring increase in melting temperature by thermal shift assay
Inhibition of PRC2 (unknown origin) using H3K27me0 as peptide substrate by LC-MS based analysis
Inhibition of His tagged EED (1 to 441) (unknown origin) using biotin-H3K27me3 peptide as substrate by AlphaScreen competition binding assay
Antagonist activity against alpha2a adrenergic receptor (unknown origin)
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human Phosphodiesterase 4D
Assay data:3 Active, 4 Tested
Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Assay data:5 Active, 4 Activity ≤ 1 µM, 11 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 5 Tested
Oral bioavailability in Sprague-Dawley rat at 2 mg/kg
Assay data:4 Tested
SummaryPubMed Citation
Terminal half life in Sprague-Dawley rat at 2 mg/kg, po
Assay data:2 Tested
Dose normalized AUC in Sprague-Dawley rat at 2 mg/kg, po
Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco-2 cells at 10 uM incubated for 2 hrs by LC/MS/MS analysis
Permeability across apical to basolateral side in human Caco-2 cells at 10 uM incubated for 2 hrs by LC/MS/MS analysis
High throughput solubility of the compound at pH 6.8 after 16 to 24 hrs by MS/MS analysis
Assay data:1 Active, 9 Tested
SummaryCompounds, ActivePubMed Citation
Lipophilicity, logD of the compound at pH 7.4 by LC with tandem MS analysis
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
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