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Inhibition of TRPV1 (unknown origin) upto 100 uM
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Modulation of TRPV1 (unknown origin) by fluorometric imaging plate reader analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at rat TRPV1
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of TRPV1 (unknown origin)
Assay data:4 Active, 3 Activity ≤ 1 µM, 9 Tested
TRPV1 Inhibition Assay from US Patent US11845730: "1,3-substituted cyclobutyl derivatives and uses thereof"
Assay data:118 Active, 6 Activity ≤ 1 nM, 108 Activity ≤ 1 µM, 118 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Potency index, ratio of SB-705498 IC50 to test compound IC50 for antagonist activity at human TRPV1 expressed in CHO cells
Assay data:1 Tested
Antagonist activity at human TRPV1 expressed in CHO cells assessed as low pH-induced Ca2+ influx at 10 uM incubated for 30 mins at pH 5 by FLIPR method
Assay data:14 Tested
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced Ca2+ influx incubated for 30 mins by FLIPR method
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced Ca2+ influx at 10 uM incubated for 30 mins by FLIPR method
Assay data:83 Tested
Agonist activity at human TRPV1
Agonist activity at TRPV1 in C57BL/6 mouse DRG neuron assessed as desensitization of TRPV1 current at 10 uM at 0 mV holding potential with continuous drug application by whole-cell patch clamp assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as induction of calcium influx by measuring increase in intracellular fluorescence intensity at 1 uM measured for 180 sec by Fluo-8 based calcium imaging analysis relative to ionomycin
Assay data:2 Active, 3 Tested
Agonist activity at mouse TRPV1 expressed in HEK293 cells assessed as activation of TRPV1 current by measuring efficacy at 1 uM at 0 mV holding potential by whole-cell patch clamp assay relative to capsaicin
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as desensitization of TRPV1 current at 1 uM at 0 mV holding potential with continuous drug application by whole-cell patch clamp assay
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as desensitization of TRPV1 current at 1 uM at 0 mV holding potential with repetitive drug application by whole-cell patch clamp assay
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as activation of TRPV1 current at 1 uM at 0 mV holding potential by whole-cell patch clamp assay relative to capsaicin
Assay data:2 Active, 5 Tested
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium accumulation preincubated with compound followed by capsaicin addition and measured at 180 sec by fluorescence based microplate reader analysis relative to control
Assay data:3 Active, 1 Activity ≤ 1 µM, 10 Tested
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium accumulation at 100 nM preincubated with compound followed by capsaicin addition and measured at 180 sec by fluorescence based microplate reader analysis relative to control
Assay data:10 Tested
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium accumulation measured at 180 sec by fluorescence based microplate reader analysis
Assay data:25 Active, 20 Activity ≤ 1 µM, 43 Tested
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium accumulation by measuring efficacy at 100 nM measured at 180 sec by fluorescence based microplate reader analysis relative to capsaicin
Assay data:44 Tested
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