Compile Data Set for Download or QSAR
Report error Found 4 Enz. Inhib. hit(s) with Target = 'Neuronal acetylcholine receptor subunit alpha-4/beta-2' and Ligand = 'BDBM221048'
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM221048(US9303017, Varenicline | US9284322, varenicline)
Affinity DataEC50:  950nMAssay 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
In Depth
Date in BDB:
4/10/2017
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM221048(US9303017, Varenicline | US9284322, varenicline)
Affinity DataIC50: 94nMAssay 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
In Depth
Date in BDB:
4/10/2017
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM221048(US9303017, Varenicline | US9284322, varenicline)
Affinity DataKi:  0.0400nMAssay Description:Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in CHOK1 cell membrane by microbeta scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM221048(US9303017, Varenicline | US9284322, varenicline)
Affinity DataKi:  0.120nM ΔG°:  -52.6kJ/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
In Depth
Date in BDB:
4/10/2017
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)