Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 54 hits in this display
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 0.480nM ΔG°: -49.4kJ/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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 2.5nM ΔG°: -45.6kJ/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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 28nM ΔG°: -40.1kJ/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
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Ki: 32.5nMAssay Description:Displacement of [125I]iodoMLA from rat cerebral cortex alpha7 nAChR at 50 nM incubated for 2 hrs by microplate scintillation assayMore data for this Ligand-Target Pair
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 37nM ΔG°: -39.4kJ/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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Ki: 37nMAssay 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
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 40nMAssay Description:Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in IMR32 cell membrane by microbeta scintillation counting methodMore data for this Ligand-Target Pair
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 94nM ΔG°: -37.3kJ/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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
Ki: 390nM ΔG°: -34.0kJ/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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Ki: 617nMAssay Description:Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]alpha-bungarotoxinMore data for this Ligand-Target Pair
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Ki: 3.54E+3nMAssay Description:Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha1 beta gamma delta of electroplaxMore data for this Ligand-Target Pair
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Ki: 3.54E+3nMAssay Description:Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]alpha-bungarotoxinMore data for this Ligand-Target Pair
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
IC50: 39nMAssay Description:Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liq...More data for this Ligand-Target Pair
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
IC50: >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
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
EC50: 1.10E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liqui...More data for this Ligand-Target Pair
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
EC50: 950nMAssay 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
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
BDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
BDBM221048(US9284322, varenicline | US9303017, Varenicline)
EC50: 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
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