BDBM50166908 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene; dihydrochloride::CHEMBL556954::US9993465, Varenicline::VARENICLINE
SMILES C1C2CNCC1c1cc3nccnc3cc21
InChI Key InChIKey=JQSHBVHOMNKWFT-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 39 hits for monomerid = 50166908
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 0.0600nMAssay Description:Binding affinity to alpha4beta2 nAChR in rat cortexMore data for this Ligand-Target Pair
3D Structure (crystal)TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 0.110nMAssay Description:Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotineMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by PDSP Ki Database
Research Triangle Institute
Curated by PDSP Ki Database
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 0.130nMAssay 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))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 0.295nMAssay Description:Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 0.400nMAssay Description:Binding affinity to alpha4beta2 nAChRMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-2(Homo sapiens (Human))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 0.480nMAssay Description:Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.H...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
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataKi: 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
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataKi: 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
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 125nMAssay Description:Displacement of [3H]epibatidine from alpha7 nicotinic receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataKi: 125nMAssay Description:Binding affinity to rat alpha7 nACHR at 10 uMMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 240nMAssay Description:Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]epibatidineMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataKi: 300nMAssay Description:Binding affinity to rat alpha7 nAChR expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataKi: 322nMAssay Description:Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha-7 subunit in rat GH4C1 cellsMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataKi: 460nMAssay 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-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 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
TargetAcetylcholine receptor subunit alpha/beta/delta/gamma(Torpedo californica)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataKi: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataEC50: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataEC50: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 94nMAssay 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))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataEC50: 0.0600nMAssay Description:Partial agonist activity at alpha4beta 2 nAChRMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 2.10E+4nMAssay Description:Agonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as stimulation of [86Rb+] efflux after 2 mins by liquid scintillation co...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University
US Patent
Georgetown University
US Patent
Affinity DataEC50: 5.50E+4nMAssay Description:Agonist activity at rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current by two-electro...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 38.9nMAssay 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataEC50: 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataEC50: 950nMAssay 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))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 94nMAssay 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-7(Rattus norvegicus (Rat))
Research Triangle Institute
Curated by ChEMBL
Research Triangle Institute
Curated by ChEMBL
Affinity DataEC50: 1.80E+4nMAssay Description:Agonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes by two-electrode voltage clamp assayMore data for this Ligand-Target Pair