Compile Data Set for Download or QSAR
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 54 hits in this display   

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM221048(US9284322, varenicline | US9303017, 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  0.0600nMAssay Description:Binding affinity to alpha4beta2 nAChR in rat cortexMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  0.120nM ΔG°:  -56.6kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM221048(US9284322, varenicline | US9303017, 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
TargetNeuronal acetylcholine receptor subunit alpha-4(Rattus norvegicus (Rat))
Research Triangle Institute

Curated by PDSP Ki Database
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  0.120nMMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  0.120nMMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to alpha4beta2 nAChRMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-2(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-2(Homo sapiens (Human))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-2(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  2.5nMMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  32.5nMpH: 7.4Assay Description:Adult male rat cerebral cortices (Pel-Freez Biologicals, Rogers, Ark.) were homogenized (polytron) in 39 volumes of ice-cold 50 mM Tris buffer (assay...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  94nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-7(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  125nMAssay Description:Displacement of [3H]epibatidine from alpha7 nicotinic receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  125nMAssay Description:Binding affinity to rat alpha7 nACHR at 10 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  300nMAssay Description:Binding affinity to rat alpha7 nAChR expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataKi:  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
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataKi:  390nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM221048(US9284322, varenicline | US9303017, 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
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
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
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
Affinity DataEC50:  0.0600nMAssay Description:Partial agonist activity at alpha4beta 2 nAChRMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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-3/beta-4(Rattus norvegicus (Rat))
Georgetown University

US Patent
LigandPNGBDBM221048(US9284322, varenicline | US9303017, Varenicline)
Affinity DataEC50:  2.20E+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
In DepthDetails US Patent
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM50166908(5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca...)
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
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Suven Life Sciences

Curated by ChEMBL
LigandPNGBDBM221048(US9284322, varenicline | US9303017, 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
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