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Binding to Nicotinic Receptor Subtypes from US Patent US11667638: "4-substitued cytisine analogues"
Assay data:50 Active, 3 Activity ≤ 1 nM, 50 Activity ≤ 1 µM, 50 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human alpha6/alpha3beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human alpha4beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Inhibition of human alpha3beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Inhibition of human alpha2beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Antagonist activity at human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential at 100 nM by two-electrode voltage clamp method
Antagonist activity at human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential in presence of BAPTA-AM at 10 uM by two-electrode voltage clamp method
Antagonist activity at human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential at 10 uM by two-electrode voltage clamp method
Antagonist activity at human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential at 1 uM by two-electrode voltage clamp method
Antagonist activity at human alpha3beta4 nAChR in SH-SY5Y cells assessed as inhibition of calcium flux by FLIPR assay
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human alpha3beta4 nAChR in SH-SY5Y cells assessed as inhibition of calcium flux at 10 uM by FLIPR assay
Assay data:8 Tested
Displacement of [3H]-epibatidine from human alpha3beta4 nAChR expressed in SH-EP1 cells membrane assessed as inhibition constant preincubated for 5 mins followed by overnight incubation with [3H]-epibatidine by gamma liquid scintilation counting analysis
Assay data:24 Active, 18 Activity ≤ 1 µM, 24 Tested
Antagonist activity at rat alpha6/alpha3beta4 nAChR
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at rat alpha6/alpha3beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at 10^-5 M at -70 mV holding potential preincubated for 5 mins followed by Ach stimulation by voltage-clamp based electrophysiological method relative to control
Antagonist activity at rat alpha6/alpha3beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential preincubated for 5 mins followed by Ach stimulation by voltage-clamp based electrophysiological method
Assay data:3 Active, 2 Activity ≤ 1 µM, 7 Tested
Inhibition of human alpha6/alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method
Assay data:2 Tested
Inhibition of human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method
Inhibition of human alpha2beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method
Nicotinic Acetylcholine alpha3beta4 Eurofins-Panlabs radioligand binding assay
Assay data:5 Tested
SummaryRelated BioAssays by Target
NACH/H Eurofins SafetyScreen44 (BI)
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