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QSS Assist FP assay from US Patent US10538528: "5H-pyrrolo[2,3-D]pyrimidin-6(7H)-one derivative"
Assay data:35 Active, 16 Activity ≤ 1 nM, 35 Activity ≤ 1 µM, 35 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Stabilization of FKBP12/RyR1 protein-protein interaction in human 8220 myoblast-derived myotubes assessed as reversal of SIN1-induced intracellular calcium leakage at 150 nM preincubated for 12 hrs followed by SIN1 stimulation and measured after 6 hrs by fura-2 AM dye based fluorescence assay relative to control
Assay data:6 Active, 16 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Effect on FKBP12/RyR1 protein-protein interaction in human myotubes by in situ proximity ligation assay
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Stabilization of FKBP12/RyR1 protein-protein interaction in human myotubes assessed as reversal of SIN1-induced reduction in FKBP12/RyR1 co-localization at 150 nM by in situ proximity ligation assay relative to control
Stabilization of FKBP12/RyR1 protein-protein interaction in human myotubes assessed as reversal of SIN1-induced reduction in FKBP12/RyR1 co-localization by measuring increase in FKBP12/RyR1 co-localization at 150 nM by in situ proximity ligation assay relative to control
Assay data:1 Tested
Displacement of [3H]ryanodine from wild type RyR3 (unknown origin) stably expressed in HEK293 cells microsomes at 10 uM by radioligand binding assay
Assay data:4 Tested
Displacement of [3H]ryanodine from wild type RyR2 (unknown origin) stably expressed in HEK293 cells microsomes at 10 uM by radioligand binding assay
Inhibition of wild type RyR3 (unknown origin) stably expressed in HEK293 cells coexpressing R-CEPIA1er assessed as suppression in caffeine-activated Ca2+ leakage from ER at 10 uM compound addition at 100 secs and measured every 10 secs for 300 secs by fluorometric analysis
Assay data:4 Active, 4 Tested
Inhibition of wild type RyR2 (unknown origin) stably expressed in HEK293 cells coexpressing R-CEPIA1er assessed as Ca2+ leakage from ER at 10 uM compound addition at 100 secs and measured every 10 secs for 300 secs by fluorometric analysis
Assay data:3 Tested
Human RyR1 (Ryanodine receptors)
Assay data:9 Active, 9 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Human RyR3 (Ryanodine receptors)
Assay data:7 Active, 7 Tested
Human RyR2 (Ryanodine receptors)
Assay data:8 Active, 8 Tested
Induction of calstabin-2 binding to PKA-phosphorylated RyR1 in mouse skeletal muscle at >50 nM
Assay data:1 Active, 1 Tested
Induction of calstabin-1 binding to PKA-phosphorylated RyR1 in mouse skeletal muscle at >50 nM
Induction of calstabin-2 binding to RyR1 in mouse skeletal muscle at >50 nM
Induction of calstabin-1 binding to RYR1 in myocardial infarction-induced heart failure calsiabin2-/- mouse soleus muscle at 0.5 mg/kg/day dosed via implantable osmotic minipumps
Inhibition of of PKA-induced RyR1 phosphorylation in myocardial infarction-induced heart failure mouse soleus muscle at 0.5 mg/kg/day dosed via implantable osmotic minipumps
Induction of calstabin-1 binding to RYR1 in myocardial infarction-induced heart failure wild type mouse soleus muscle at 0.5 mg/kg/day dosed via implantable osmotic minipumps
Induction of calstabin-2 binding to RyR2 P2328S mutant (unknown origin) at 0.1 umol/L
Effect on baseline channel function of RyR2 (unknown origin) at 0.1 umol/L
SummaryRelated BioAssays by Target
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