Found 12 Enz. Inhib. hit(s) with Target = 'Neuronal acetylcholine receptor subunit alpha-4/beta-2' and Ligand = 'BDBM50382474' TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.0620nM ΔG°: -54.2kJ/molepH: 7.4 T: 2°CAssay Description:Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris....More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.0620nMAssay Description:Displacement of [3H]epibatidine from human alpha4beta2 nAChR after 4 hrs by cell-based assayMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataIC50: 4.80nMAssay Description:Antagonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells assessed as inhibition of carbamylcholine induced 86Rb+ ion efflux preincuba...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataIC50: 7.5nMAssay Description:IC50(10′): The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataIC50: 11nMAssay Description:Antagonist activity at human alpha4beta2 nAChR assessed as inhibition of nicotine-induced [86Rb+] efflux preincubated for 10 mins before nicotine exp...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataIC50: 11nMAssay Description:Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataIC50: 12nMAssay Description:IC50(10′): The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 24nMAssay Description:Agonist activity at human alpha4beta2 nAChR assessed as stimulation of [86Rb+] efflux after 2 mins by cell-based liquid scintillation countingMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 24nMAssay Description:The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β2 nAChR subtypes....More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 24nMAssay Description:Agonist activity at human alpha4beta2 nACHR expressed in HEK293 cells assessed as stimulation of 86Rb+ efflux after 2 hrs by liquid scintillation cou...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 5.80nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells assessed as 86Rb+ ion efflux after 9.5 mins by flip-plate techniqueMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 0.270nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in rat GH4C1 cells assessed as induction of peak current amplitude at holding potential of -70 ...More data for this Ligand-Target Pair
