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Inhibition of Nav1.6 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Nav1.2 (unknown origin)
Inhibition of human Nav1.7
Inhibition of human Nav1.5
In Vitro Assay from US Patent US9260446: "Synthetic methods for spiro-oxindole compounds"
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Guanidine Influx Assay from US Patent US9695185: "Synthetic methods for spiro-oxindole compounds"
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
Assay data:2 Active, 7 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Assay data:11 Active, 10 Activity ≤ 1 µM, 13 Tested
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Assay data:9 Active, 7 Activity ≤ 1 µM, 14 Tested
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Assay data:11 Active, 1 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 12 Tested
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Assay data:14 Active, 5 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 15 Tested
Cmax in human at 4 to 8% (w/w) administered topically as ointment for 21 consecutive days during phase-1 clinical trial
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Binding affinity to inactivated state of human Nav1.7 expressed in HEK293 cells by whole cell voltage clamp assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of human Nav1.7 expressed in HEK293 cells assessed as reduction in 14C-guanidinium influx by scintillation counting analysis
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Analgesic activity in human assessed as dental pain relief at 500 mg administered as single dose measured 4 to 12 hrs post dose
Assay data:1 Active, 1 Tested
SummaryCompounds, Active
Analgesic activity in rat model of chronic constriction injury-induced neuropathic pain assessed as reversal of pain response at 2% (w/v) administered topically as ointment measured upto 1 hr by electrovonfrey anesthesiometry
Assay data:2 Active, 3 Tested
Analgesic activity in rat model of CFA-induced chronic inflammatory pain assessed as reduction in nociceptive threshold at 200 mg/kg, po by Von Frey filament assay
Assay data:2 Active, 2 Tested
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