BDBM50382474 CHEMBL2024096::US9303017, Sazetidine-A
SMILES OCCCCC#Cc1cncc(OC[C@@H]2CCN2)c1
InChI Key InChIKey=WONBUILDJNKYCB-AWEZNQCLSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 25 hits for monomerid = 50382474
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.0620nM ΔG°: -12.9kcal/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-2/beta-2(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.0870nM ΔG°: -12.7kcal/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-3/beta-2(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.380nM ΔG°: -11.9kcal/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-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 52nM ΔG°: -9.23kcal/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-2/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 210nM ΔG°: -8.46kcal/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-7(Rattus norvegicus (Rat))
Georgetown University Medical Center
Curated by ChEMBL
Georgetown University Medical Center
Curated by ChEMBL
Affinity DataKi: 670nMAssay Description:Displacement of [3H]-Epibatidine from rat alpha7 nACHR expressed in HEK293 cell membranes membranes by liquid scintillation counting analysisMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Georgetown University Medical Center
Curated by ChEMBL
Georgetown University Medical Center
Curated by ChEMBL
Affinity DataKi: 670nM ΔG°: -7.82kcal/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-7(Rattus norvegicus (Rat))
Georgetown University Medical Center
Curated by ChEMBL
Georgetown University Medical Center
Curated by ChEMBL
Affinity DataKi: 1.60E+3nM ΔG°: -7.34kcal/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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataKi: 1.90E+3nMAssay Description:Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cells after 4 hrsMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataKi: 1.90E+3nM ΔG°: -7.25kcal/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 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 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: 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: 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 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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as inhibition of nicotine-induced [86Rb+] efflux preincubated for 10 ...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: 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
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: 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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay 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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataEC50: 2.40E+4nMAssay 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 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: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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
Curated by ChEMBL
Georgetown University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay 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