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Selectivity interaction (Eurofins CEREP Diversity Profile (receptors and ion channels)) EUB0000279b CHRNB2
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Panel of non-epigenetic targets (kinases, GPCRs, ion channels, and transporters, Eurofins) ) EUB0000271b CHRNA4
Inhibition of Nicotinic Acetylcholine alpha3beta4 at 10.0 M in the Eurofins Panlabs Safety Screen
Activity against NACH/CENT/R in the Eurofins Panlabs screen (BI) by Radioactive Assay
Agonist activity in the Eurofins SafetyScreen44 (CEREP) (BI) against N_NEURO_A4B2 by Radioligand Binding (Cerep_3029)
Assay data:4 Tested
SafetyScreen: nAChR (alpha4/beta2) Human Ion Channel Binding Agonist Radioligand LeadHunter Assay, catalogue number: 3029
Assay data:10 Tested
Displacement of [125I]-epibatidine from human recombinant nAChR alpha3beta4 receptor expressed in CHO-K1 cells assessed as inhibition constant incubated for 60 mins by spectrophotometric analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of [125I]-epibatidine from human recombinant nAChR alpha3beta4 receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
Displacement of [125I]-epibatidine from human recombinant nAChR alpha3beta4 receptor expressed in CHO-K1 cells at 10 uM incubated for 60 mins by spectrophotometric analysis relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human neuronal alpha4beta2 receptor at 10 uM by agonist radioligand based assay relative to control
Antagonist activity at human alpha4/beta2 nAChR expressed in HEK293 cells assessed as nicotine-induced intracellular calcium release incubated for 15 mins by FLIPR analysis
Assay data:11 Active, 4 Activity ≤ 1 µM, 11 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human alpha3/beta4 nAChR expressed in HEK293 cells assessed as nicotine-induced intracellular calcium release incubated for 15 mins by FLIPR analysis
Assay data:9 Active, 3 Activity ≤ 1 µM, 11 Tested
Inhibition of [3H]epibatidine from binding to human nACh receptor alpha4beta2 expressed in HEK293 cell membrane at 10 uM incubated for 2.5 hrs by liquid scintillation counting analysis relative to control
Inhibition of [3H]epibatidine from binding to rat nACh receptor alpha3beta4 expressed in HEK293 cell membrane at 10 uM incubated for 2.5 hrs by liquid scintillation counting analysis relative to control
Antagonist activity at rat alpha4beta4 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by measuring ratio of IC50 by voltage-clamp based electrophysiological assay relative to GeXIVA[1,4]
Antagonist activity at rat alpha2beta4 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by measuring ratio of IC50 by voltage-clamp based electrophysiological assay relative to GeXIVA[1,4]
Antagonist activity at rat alpha4beta2 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by measuring ratio of IC50 by voltage-clamp based electrophysiological assay relative to GeXIVA[1,4]
Antagonist activity at rat alpha2beta2 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by measuring ratio of IC50 by voltage-clamp based electrophysiological assay relative to GeXIVA[1,4]
Antagonist activity at rat alpha6/alpha3beta4 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by measuring ratio of IC50 by voltage-clamp based electrophysiological assay relative to GeXIVA[1,4]
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