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TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM82070(CAS_29790-52-1 | NICOTINE-L (BASE) | Nicotine-D sa...)
Affinity DataEC50:  2.40E+3nMAssay 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)
Georgetown University

US Patent
LigandPNGBDBM221048(US9303017, Varenicline | US9284322, 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
In Depth
Date in BDB:
4/10/2017
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50382474(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)
Georgetown University

US Patent
LigandPNGBDBM50428085(CHEMBL2323566 | US9303017, (S)-15, YL-1-127)
Affinity DataEC50:  310nMAssay 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)
Georgetown University

US Patent
LigandPNGBDBM50428079(CHEMBL2323569 | US9303017, 25, YL-1-199)
Affinity DataEC50:  160nMAssay 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)
Georgetown University

US Patent
LigandPNGBDBM50428081(CHEMBL2323570 | US9303017, (S)-17)
Affinity DataEC50:  63nMAssay 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)
Georgetown University

US Patent
LigandPNGBDBM50259713(CHEMBL4095303)
Affinity DataEC50:  1.01E+4nMAssay Description:Partial agonist activity at human alpha4beta2 nAChR expressed in GH4CL cells by whole-cell patch clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50406539(CHEMBL4175573)
Affinity DataEC50:  1.90E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in rat GH4C1 cells assessed as inward channel current amplitude at -70 mV holding potential by ...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)
Georgetown University

US Patent
LigandPNGBDBM50406688(CHEMBL4166620)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in rat GH4C1 cells assessed as inward channel current amplitude at -70 mV holding potential by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM50459884(CHEMBL4228846)
Affinity DataEC50:  660nMAssay Description:Positive allosteric modulation of human alpha2beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50459884(CHEMBL4228846)
Affinity DataEC50:  275nMAssay Description:Positive allosteric modulation of human (alpha4beta2)2beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50459884(CHEMBL4228846)
Affinity DataEC50:  446nMAssay Description:Positive allosteric modulation of human alpha4beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50229715(CHEMBL4070615)
Affinity DataEC50: >2.50E+4nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50465456(CHEMBL4283703)
Affinity DataEC50:  200nMAssay Description:Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50465457(Phantasmidine)
Affinity DataEC50:  5.60E+4nMAssay Description:Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50465458(CHEMBL1199383)
Affinity DataEC50:  2.10E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50049757((2R,4S)-2-(6-Iodo-pyridin-3-yl)-7-aza-bicyclo[2.2....)
Affinity DataEC50:  25nMAssay Description:Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50465459(CHEMBL4290888)
Affinity DataEC50:  200nMAssay Description:Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM50498032(CHEMBL3329532)
Affinity DataEC50:  1.60E+4nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498033(CHEMBL3329540)
Affinity DataEC50:  53nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498034(CHEMBL3329543)
Affinity DataEC50:  2.90E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498035(CHEMBL3329530)
Affinity DataEC50:  5.90E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498033(CHEMBL3329540)
Affinity DataEC50:  870nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498040(CHEMBL3329533)
Affinity DataEC50:  2.90E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498033(CHEMBL3329540)
Affinity DataEC50:  120nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498051(CHEMBL3329528)
Affinity DataEC50:  140nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498044(CHEMBL3329529)
Affinity DataEC50:  5.10E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498035(CHEMBL3329530)
Affinity DataEC50:  490nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498049(CHEMBL3329534)
Affinity DataEC50:  1.10E+4nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498045(CHEMBL3329537)
Affinity DataEC50:  210nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498047(CHEMBL3329539)
Affinity DataEC50:  850nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498048(CHEMBL3329541)
Affinity DataEC50:  2.10E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498052(CHEMBL3329546)
Affinity DataEC50:  1.00E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498044(CHEMBL3329529)
Affinity DataEC50:  9.70E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498041(CHEMBL3329531)
Affinity DataEC50:  850nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498040(CHEMBL3329533)
Affinity DataEC50:  1.10E+4nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498037(CHEMBL3329535)
Affinity DataEC50:  1.70E+4nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498047(CHEMBL3329539)
Affinity DataEC50:  2.80E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498048(CHEMBL3329541)
Affinity DataEC50:  3.80E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Human)
Georgetown University

US Patent
LigandPNGBDBM50498052(CHEMBL3329546)
Affinity DataEC50:  2.30E+3nMAssay Description:Agonist activity at human alpha4beta2 nAChR low sensitivity isoform transfected in SH-EP1 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498051(CHEMBL3329528)
Affinity DataEC50:  80nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498044(CHEMBL3329529)
Affinity DataEC50:  750nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498040(CHEMBL3329533)
Affinity DataEC50:  370nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498037(CHEMBL3329535)
Affinity DataEC50:  1.90E+3nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498045(CHEMBL3329537)
Affinity DataEC50:  62nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498048(CHEMBL3329541)
Affinity DataEC50:  920nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498038(CHEMBL3329542)
Affinity DataEC50:  2.00E+3nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498050(CHEMBL3329544)
Affinity DataEC50:  3.80E+3nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498053(CHEMBL3329545)
Affinity DataEC50:  540nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
LigandPNGBDBM50498052(CHEMBL3329546)
Affinity DataEC50:  100nMAssay Description:Agonist activity at human alpha6/alpha3beta2beta3 nAChR transfected in CHO cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
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