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Potency index, ratio of test compound to englerin A for agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells assessed as increase in intracellular calcium level at 1 uM measured at 5 secs interval for 300 secs in presence of TRPC4/5 antagonist Pico145 by Fura-2AM dye based fluorescence assay
Assay data:5 Tested
Agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells assessed as increase in intracellular calcium level at 0.1 uM measured at 5 secs interval for 300 secs by Fura-2AM dye based fluorescence assay
Assay data:1 Active, 5 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells assessed as increase in intracellular calcium level at 1 uM measured at 5 secs interval for 300 secs by Fura-2AM dye based fluorescence assay
Assay data:5 Active, 5 Tested
Inhibition of human TRPC1/TRPC5 expressed in HEK293 cells assessed as reduction in englerin A-induced current at 5 uM measured every 10 secs by electrophysiology assay relative to control
Assay data:1 Tested
Inhibition of human TRPC4/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human TRPC5/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Antagonist activity at TRPC4/TRPC1 in human A498 cells assessed as reduction in englerin A-induced calcium entry preincubated for 30 mins followed by englerin A addition by fluorescence method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 800 secs by Fluo-4 AM-based fluorometric assay relative to control
Assay data:1 Active, 2 Tested
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM in presence of shTRPC1 preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Assay data:1 Active, 1 Tested
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in slope at 3 to 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in peak amplitude at 3 to 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in AUC of calcium entry at 3 to 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in slope at 0.3 to 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in peak amplitude at 0.3 to 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring increase in AUC of calcium entry at 0.3 to 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Assay data:2 Tested
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Assay data:5 Active, 3 Activity ≤ 1 µM, 25 Tested
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Assay data:36 Tested
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