Compile Data Set for Download or QSAR
Report error Found 583 of ec50 for UniProtKB: P43681
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 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 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 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 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 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 50382474BDBM50382474(CHEMBL2024096 | US9303017, Sazetidine-A)
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
In Depth
Date in BDB:
11/21/2016
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 50143282BDBM50143282((1R,9R)-7,11-diazatricyclo[7.3.1.0~2,7~]trideca-2,...)
Affinity DataEC50:  0.420nMAssay 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 82070BDBM82070(CAS_29790-52-1 | NICOTINE-L (BASE) | Nicotine-D sa...)
Affinity DataEC50:  1nMAssay 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 50161088BDBM50161088(11-Bromo-1,2,3,4,5,6-hexahydro-1,5-methano-pyrido[...)
Affinity DataEC50:  1.10nMAssay 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 50216318BDBM50216318((1S,4S)-2-(6-fluoro-3-pyridinyl)-2,5-diazabicyclo[...)
Affinity DataEC50:  1.62nMAssay Description:Agonist activity at alpha-4-beta-2 in IMR-32cells assessed as calcium influx by FLIPR assayMore 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 50161084BDBM50161084(1,2,3,4,5,6-Hexahydro-1,5-methano-pyrido[1,2-a][1,...)
Affinity DataEC50:  2.20nMAssay 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 50398820BDBM50398820(CHEMBL2177538)
Affinity DataEC50:  2.30nMAssay Description:Agonist activity at human alpha4beta2 nAChR high sensitivity form expressed in human SH-EP1 cells assessed as increase in calcium flux by FLIPRMore 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 50398821BDBM50398821(CHEMBL2177537)
Affinity DataEC50:  2.30nMAssay Description:Agonist activity at human alpha4beta2 nAChR high sensitivity form expressed in human SH-EP1 cells assessed as increase in calcium flux by FLIPRMore 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 50161089BDBM50161089(11-Chloro-1,2,3,4,5,6-hexahydro-1,5-methano-pyrido...)
Affinity DataEC50:  4nMAssay 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 50549595BDBM50549595(CHEMBL4741357)
Affinity DataEC50:  5nMAssay Description:Partial agonist activity at human alpha4beta2 transfected in rat GH4-C1 cells at holding potential of -70 mV by whole cell patch clamp electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
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 50382474BDBM50382474(CHEMBL2024096 | US9303017, Sazetidine-A)
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
In Depth
Date in BDB:
2/7/2013
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 50201064BDBM50201064((1R,6S)-2-bromo-5-(3,8-diaza-bicyclo[4.2.0]oct-3-y...)
Affinity DataEC50:  6.10nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50437504BDBM50437504(CHEMBL2409631)
Affinity DataEC50:  6.20nMAssay Description:Agonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintil...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
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 50201055BDBM50201055((1R,6S)-3-(6-chloro-5-methylpyridin-3-yl)-3,8-diaz...)
Affinity DataEC50:  7.20nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50201048BDBM50201048((1R,6S)-3-(5,6-dibromopyridin-3-yl)-3,8-diaza-bicy...)
Affinity DataEC50:  7.80nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50398321BDBM50398321(CHEMBL2177344)
Affinity DataEC50:  8.80nMAssay Description:Agonist activity at high sensitivity and low sensitivity alpha4beta2-nAChR expressed in human SH-EP1 cells by 86Rb+ ion flux assayMore 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 50328016BDBM50328016(3-[(2(S)-Pyrrolidinyl)methoxy]-5-phenylaminopyridi...)
Affinity DataEC50:  10nMAssay Description:Agonist activity at human nAChR alpha4beta2 in human SH-EP1 cells assessed as induction in rubidium effluxMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
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 50382466BDBM50382466(CHEMBL2024087)
Affinity DataEC50:  10.2nMAssay 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
In Depth
Date in BDB:
2/7/2013
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 50398320BDBM50398320(CHEMBL2177345)
Affinity DataEC50:  11.3nMAssay Description:Agonist activity at high sensitivity and low sensitivity alpha4beta2-nAChR expressed in human SH-EP1 cells by 86Rb+ ion flux assayMore 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 50398820BDBM50398820(CHEMBL2177538)
Affinity DataEC50:  12nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity form expressed in human SH-EP1 cells assessed as increase in calcium flux by FLIPRMore 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 50201061BDBM50201061((1R,6S)-3-(5,6-dichloro-pyridin-3-yl)-3,8-diaza-bi...)
Affinity DataEC50:  12nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50114004BDBM50114004(CHEMBL3603947)
Affinity DataEC50:  13nMAssay 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
In Depth
Date in BDB:
11/21/2016
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 50201062BDBM50201062((1R,6S)-3-(6-chloro-pyridin-3-yl)-3,8-diaza-bicycl...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50437503BDBM50437503(CHEMBL2409627)
Affinity DataEC50:  14nMAssay Description:Agonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintil...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
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 50382467BDBM50382467(CHEMBL2024089)
Affinity DataEC50:  15.7nMAssay 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
In Depth
Date in BDB:
2/7/2013
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 50210334BDBM50210334(CHEMBL3948977)
Affinity DataEC50:  16nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells after 9.5 mins by 86Rb+ efflux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/8/2018
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 50210334BDBM50210334(CHEMBL3948977)
Affinity DataEC50:  16nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells after 9.5 mins by 86Rb+ efflux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/8/2018
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 50210335BDBM50210335(CHEMBL3898434)
Affinity DataEC50:  17nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells after 9.5 mins by 86Rb+ efflux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/8/2018
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:  17nMAssay Description:Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/5/2012
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 50210335BDBM50210335(CHEMBL3898434)
Affinity DataEC50:  17nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells after 9.5 mins by 86Rb+ efflux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/8/2018
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 50382472BDBM50382472(CHEMBL2024094)
Affinity DataEC50:  17.5nMAssay 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
In Depth
Date in BDB:
2/7/2013
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 50437496BDBM50437496(CHEMBL3037927)
Affinity DataEC50:  18nMAssay Description:Agonist activity at alpha4beta2 nACHR in human SHEP1 cell membranes assessed as stimulation of calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
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 50382472BDBM50382472(CHEMBL2024094)
Affinity DataEC50:  18nMAssay Description:Agonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintil...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
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 50382468BDBM50382468(CHEMBL2024090)
Affinity DataEC50:  18.2nMAssay 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
In Depth
Date in BDB:
2/7/2013
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 50398319BDBM50398319(CHEMBL2177346)
Affinity DataEC50:  19.1nMAssay Description:Agonist activity at high sensitivity and low sensitivity alpha4beta2-nAChR expressed in human SH-EP1 cells by 86Rb+ ion flux assayMore 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 50201072BDBM50201072((1R,6S)-3-(6-bromo-5-methoxy-pyridin-3-yl)-3,8-dia...)
Affinity DataEC50:  21nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50437502BDBM50437502(CHEMBL2409625)
Affinity DataEC50:  23nMAssay Description:Agonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintil...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
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 50382469BDBM50382469(CHEMBL2024091)
Affinity DataEC50:  23.3nMAssay 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
In Depth
Date in BDB:
2/7/2013
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 50382474BDBM50382474(CHEMBL2024096 | US9303017, Sazetidine-A)
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
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 50411219BDBM50411219(CHEMBL479614)
Affinity DataEC50:  24nMAssay Description:Agonist activity at human alpha4beta2 ACHR expressed in HEK293 cells assessed as change in intracellular calcium concentration by FLIPRMore 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 50382474BDBM50382474(CHEMBL2024096 | US9303017, Sazetidine-A)
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
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 50419266BDBM50419266(CHEMBL1835610)
Affinity DataEC50:  25nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as increase of carbamylcholine-induced 86Rb+ ion efflux by liqui...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2012
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 DataEC50:  27nMAssay Description:Agonist activity at alpha-4-beta-2 in IMR-32cells assessed as calcium influx by FLIPR assayMore 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 50399420BDBM50399420(CHEMBL2178336)
Affinity DataEC50:  28nMAssay 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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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