Compile Data Set for Download or QSAR
Report error Found 2139 for UniProtKB: P17787
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataEC50:  0.00880nMAssay Description:Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0100nMAssay Description:Potency to displace [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 immuno-isolated from M10 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50216315BDBM50216315((1R,4R)-2-(6-chloro-3-pyridinyl)-2,5-diazabicyclo[...)
Affinity DataKi:  0.0180nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50406803BDBM50406803(CHEMBL4168511)
Affinity DataKi:  0.0200nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataEC50:  0.0200nMAssay Description:Agonist activity at alpha4beta 2 nAChRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50143320BDBM50143320(2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]hept...)
Affinity DataKi:  0.0260nMAssay Description:Displacement of [3H]epibatidine from alpha-4-beta-2 nAChRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50123270BDBM50123270(azidoepibatidine | 2-(5-Azido-6-chloro-pyridin-3-y...)
Affinity DataKi:  0.0270nMAssay Description:Binding affinity to alpha4 beta-2 receptor subtype from mouse fibroblast M10 cells was measured using [3 H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50143314BDBM50143314(CHEMBL298826 | (+)-Epibatidine | 2-(6-Chloro-pyrid...)
Affinity DataKd:  0.0300nMAssay Description:Binding affinity to alpha4beta2 nACh receptor (unknown origin) expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2017
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-2(Human)
University of Illinois At Chicago

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKd:  0.0300nMAssay Description:Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0330nMAssay Description:Displacement of [3H]epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-2(Human)
University of Illinois At Chicago

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0350nMAssay Description:Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0350nMAssay Description:Binding affinity to alpha4 beta-2 receptor subtype from mouse fibroblast M10 cells was measured using [3 H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50161086BDBM50161086(9-Iodo-1,2,3,4,5,6-hexahydro-1,5-methano-pyrido[1,...)
Affinity DataEC50:  0.0360nMAssay Description:Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50079453BDBM50079453(2-(6-Chloro-pyridin-3-yl)-7-methyl-7-aza-bicyclo[2...)
Affinity DataKi:  0.0380nMAssay Description:Displacement of [3H]epibatidine from alpha-4-beta-2 nAChRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049750BDBM50049750(CHEMBL59986 | (S)-3-(azetidin-2-ylmethoxy)pyridine...)
Affinity DataKi:  0.0400nMAssay Description:Binding affinity to alpha4beta2 nAChR in human brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049750BDBM50049750(CHEMBL59986 | (S)-3-(azetidin-2-ylmethoxy)pyridine...)
Affinity DataKi:  0.0400nMAssay Description:Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2020
Entry Details Article

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049750BDBM50049750(CHEMBL59986 | (S)-3-(azetidin-2-ylmethoxy)pyridine...)
Affinity DataKi:  0.0400nMAssay Description:Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/9/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50110258BDBM50110258(2-(6-Chloro-pyridin-3-yl)-9-aza-bicyclo[4.2.1]non-...)
Affinity DataKi:  0.0400nMAssay Description:Displacement of [3H]epibatidine from nAChR alpha4beta2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 221048BDBM221048(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)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50143320BDBM50143320(2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]hept...)
Affinity DataKi:  0.0450nMAssay Description:Binding affinity to alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2016
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 82070BDBM82070(CAS_29790-52-1 | NICOTINE-L (BASE) | Nicotine-D sa...)
Affinity DataKi:  0.0450nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0460nMAssay Description:Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049750BDBM50049750(CHEMBL59986 | (S)-3-(azetidin-2-ylmethoxy)pyridine...)
Affinity DataKi:  0.0500nMAssay Description:Binding affinity against human Nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50143279BDBM50143279((S)-2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]...)
Affinity DataKi:  0.0500nMAssay Description:Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/19/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50161085BDBM50161085(9-Bromo-1,2,3,4,5,6-hexahydro-1,5-methano-pyrido[1...)
Affinity DataEC50:  0.0500nMAssay Description:Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0500nMAssay Description:Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049750BDBM50049750(CHEMBL59986 | (S)-3-(azetidin-2-ylmethoxy)pyridine...)
Affinity DataKi:  0.0520nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50062641BDBM50062641(CHEMBL430497 | 5-((R)-1-Azetidin-2-ylmethoxy)-2-ch...)
Affinity DataKi:  0.0550nMAssay Description:Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/9/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50062641BDBM50062641(CHEMBL430497 | 5-((R)-1-Azetidin-2-ylmethoxy)-2-ch...)
Affinity DataKi:  0.0550nMAssay Description:Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/9/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0558nMAssay Description:Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166908BDBM50166908(CHEMBL556954 | VARENICLINE | 5,8,14-triazatetracyc...)
Affinity DataKi:  0.0600nMAssay Description:Binding affinity to alpha4beta2 nAChR in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0600nMAssay Description:Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human K177 cell membrane incubated for 75 mins by liquid scintillation spectro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0600nMAssay Description:Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human K177 cell membrane incubated for 75 mins by liquid scintillation spectro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166908BDBM50166908(CHEMBL556954 | VARENICLINE | 5,8,14-triazatetracyc...)
Affinity DataEC50:  0.0600nMAssay Description:Partial agonist activity at alpha4beta 2 nAChRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 397477BDBM397477(US9993465, Sazetidine-A)
Affinity DataKi:  0.0620nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2020
Entry Details
US Patent

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50382474BDBM50382474(CHEMBL2024096 | US9303017, Sazetidine-A)
Affinity DataKi:  0.0620nM ΔG°:  -54.2kJ/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
US Patent

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50049757BDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataKi:  0.0700nMAssay Description:Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2020
Entry Details Article

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50194072BDBM50194072(syn-7-(6-chloro-pyridin-3-yl)-2-azabicyclo[2.2.1]h...)
Affinity DataKi:  0.0785nMAssay Description:Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-2/beta-2(Human)
Georgetown University

US Patent
LigandChemical structure of BindingDB Monomer ID 397477BDBM397477(US9993465, Sazetidine-A)
Affinity DataKi:  0.0870nMAssay 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
In Depth
Date in BDB:
5/5/2020
Entry Details
US Patent

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50119791BDBM50119791(1-Decyl-3-((S)-1-methyl-pyrrolidin-2-yl)-pyridiniu...)
Affinity DataKi:  0.0900nMAssay Description:Binding affinity to alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2016
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50398821BDBM50398821(CHEMBL2177537)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]nicotine from human alpha4beta2 nAChR expressed in human SH-EP1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50174139BDBM50174139(6-methyl-5,7,13-triazatetracyclo[9.3.1.02,10.04,8]...)
Affinity DataKi:  0.100nMAssay Description:Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50397944BDBM50397944(CHEMBL2177512)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]nicotine from human alpha4beta2 nAChR expressed in human SH-EP1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50174152BDBM50174152(4,5-Dichloro-10-aza-tricyclo[6.3.1.0*2,7*]dodeca-2...)
Affinity DataKi:  0.100nMAssay Description:Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50161090BDBM50161090(9-Chloro-1,2,3,4,5,6-hexahydro-1,5-methano-pyrido[...)
Affinity DataEC50:  0.110nMAssay Description:Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166908BDBM50166908(CHEMBL556954 | VARENICLINE | 5,8,14-triazatetracyc...)
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
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 221048BDBM221048(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
US Patent
PDB3D3D Structure (crystal)
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50174145BDBM50174145(6-methyl-7-thia-5,13-diazatetracyclo[9.3.1.02,10.0...)
Affinity DataKi:  0.120nMAssay Description:Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166908BDBM50166908(CHEMBL556954 | VARENICLINE | 5,8,14-triazatetracyc...)
Affinity DataKi:  0.120nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2020
Entry Details
US Patent

TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
National Institute of Diabetes and Digestive and Kidney Diseases

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50174148BDBM50174148(5-methyl-7-oxa-6,13-diazatetracyclo[9.3.1.02,10.04...)
Affinity DataKi:  0.130nMAssay Description:Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
Displayed 1 to 50 (of 2139 total ) | Next | Last >>
Jump to: