varenicline [Ligand Id: 5459] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1396 (Chantix, CP-526555, CP-526,555, Varenicline)
  • nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human [ChEMBL: CHEMBL1907588] [GtoPdb: 462475471476] [UniProtKB: P02708P07510P11230Q07001]
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  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
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  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Rat [ChEMBL: CHEMBL1907590] [GtoPdb: 463474] [UniProtKB: P12389P12392]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit in Human [GtoPdb: 464472] [UniProtKB: P32297P17787]
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat [ChEMBL: CHEMBL1907593] [GtoPdb: 464474] [UniProtKB: P04757P12392]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Human [ChEMBL: CHEMBL1907591] [GtoPdb: 474465] [UniProtKB: P30926P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat [ChEMBL: CHEMBL1907595] [GtoPdb: 465474] [UniProtKB: P09483P12392]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptors; alpha-3/beta-4, alpha-5, beta-2 in Human [ChEMBL: CHEMBL2221346] [GtoPdb: 472466474464] [UniProtKB: P17787P30532P30926P32297]
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  • nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor α6 subunit/Neuronal acetylcholine receptor subunit alpha-6/beta-3 in Rat [ChEMBL: CHEMBL3883329] [GtoPdb: 473467] [UniProtKB: P12391P43143]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907588] [GtoPdb: 462475471476] [UniProtKB: P02708P07510P11230Q07001]
ChEMBL Binding affinity to alpha-1-beta-gamma-delta nicotinic receptor B 5.09 pKi 8200 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4749-4752 [PMID:20663668]
ChEMBL Antagonist activity at human alpha1beta1gammadelta nAChR expressed in human TE671/RD cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 6 pIC50 >1000 nM IC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Agonist activity at human alpha1beta1gammadelta nAChR expressed in human TE671/RD cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 6 pEC50 >1000 nM EC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha2beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 9.32 pKi 0.48 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]epibatidine from rat alpha2beta2 nAChR expressed in HEK293 cells after 4 hrs B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907590] [GtoPdb: 463474] [UniProtKB: P12389P12392]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha2beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 7.03 pKi 94 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells after 4 hrs B 7.15 pKi 71 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit in Human [GtoPdb: 464472] [UniProtKB: P32297P17787]
GtoPdb - - 7.4 pKi 39.6 nM Ki J. Med. Chem. (2020) 63: 2833-2853 [PMID:32026697]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha3beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 8.6 pKi 2.5 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta2 nAChR expressed in HEK293 cells after 4 hrs B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
ChEMBL Binding affinity to alpha3beta4 nAChR B 7.07 pKi 86 nM Ki J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Displacement of [3H]epibatidine from alpha3beta4 nicotinic receptor expressed in human HEK293 cells B 7.13 pKi 74.7 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4749-4752 [PMID:20663668]
GtoPdb - - 7.4 pKi 39.6 nM Ki J. Med. Chem. (2020) 63: 2833-2853 [PMID:32026697]
ChEMBL Antagonist activity at human alpha3beta4 nAChR expressed in human SH-SY5Y cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 6 pIC50 >1000 nM IC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Inhibition of human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay B 6.96 pIC50 110 nM IC50 J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Agonist activity at human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay F 5.85 pEC50 1400 nM EC50 J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Agonist activity at human alpha3beta4 nAChR expressed in human SH-SY5Y cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 6 pEC50 >1000 nM EC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907593] [GtoPdb: 464474] [UniProtKB: P04757P12392]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs B 6.34 pKi 460 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 6.41 pKi 390 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nACHR B 7.07 pKi 86 nM Ki J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Displacement of [3H]epibatidine from rat forebrain alpha3beta4 nAChR by competition binding assay B 7.07 pKi 86 nM Ki ACS Med. Chem. Lett. (2014) 5: 1196-1201 [PMID:25408831]
ChEMBL Desensitization of rat alpha3beta4 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as inhibition of nicotine-induced [86Rb+] efflux preincubated for 10 mins before nicotine exposure by liquid scintillation counting B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Agonist activity at rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current by two-electrode voltage clamp electrophysiological analysis B 4.26 pEC50 55000 nM EC50 J. Med. Chem. (2014) 57: 836-848 [PMID:24428686]
ChEMBL Agonist activity at rat alpha3beta4 nACHR expressed in HEK293 cells assessed as stimulation of 86Rb+ efflux after 2 hrs by liquid scintillation counting analysis B 4.68 pEC50 21000 nM EC50 J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Agonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as stimulation of [86Rb+] efflux after 2 mins by liquid scintillation counting B 4.68 pEC50 21000 nM EC50 J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
ChEMBL Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]alpha-bungarotoxin B 5.45 pKi 3540 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]alpha-bungarotoxin B 6.21 pKi 617 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]epibatidine B 6.62 pKi 240 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Binding affinity to alpha4beta2 nAChR B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cells B 9.53 pKi 0.29 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4749-4752 [PMID:20663668]
ChEMBL Displacement of [3H]epibatidine from human alpha4beta2 nAChR after 4 hrs by cell-based assay B 9.89 pKi 0.13 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotine B 9.96 pKi 0.11 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-4897 [PMID:16171993]
GtoPdb Binding affinity to human nicotinic acetylcholine receptor α4β2 expressed in IMR32 cells using [3H]epibatidine radioligand. - 9.96 pKi 0.11 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-97 [PMID:16171993]
ChEMBL Binding affinity to alpha4beta2 nAChR in rat cortex B 10.22 pKi 0.06 nM Ki J. Med. Chem. (2013) 56: 593-624 [PMID:23121096]
GtoPdb In vitro affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [3H]-(−)-cytisine. - 10.4 pKi 0.04 nM Ki J. Med. Chem. (2020) 63: 2833-2853 [PMID:32026697]
ChEMBL Inactivation of alpha4beta2* nAChR low affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis B 7.03 pIC50 94 nM IC50 J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Antagonist activity at human alpha4beta2 nAChR assessed as inhibition of nicotine-induced [86Rb+] efflux preincubated for 10 mins before nicotine exposure by cell-based liquid scintillation counting B 7.03 pIC50 94 nM IC50 J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Inactivation of alpha4beta2* nAChR high affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 7.15 pIC50 70 nM IC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 7.41 pIC50 39 nM IC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 7.41 pIC50 38.9 nM IC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Activation of alpha4beta2* nAChR high affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 5.85 pEC50 1400 nM EC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 5.96 pEC50 1096.48 nM EC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting F 5.96 pEC50 1096 nM EC50 J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
ChEMBL Agonist activity at human alpha4beta2 nACHR expressed in HEK293 cells assessed as stimulation of 86Rb+ efflux after 2 hrs by liquid scintillation counting analysis B 6.02 pEC50 950 nM EC50 J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Agonist activity at human alpha4beta2 nAChR assessed as stimulation of [86Rb+] efflux after 2 mins by cell-based liquid scintillation counting B 6.02 pEC50 950 nM EC50 J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Agonist activity at human alpha4beta2 nAChR expressed in xenopus oocytes by electrophysiology method B 8.64 pEC50 2.3 nM EC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Partial agonist activity at alpha4beta 2 nAChR F 10.22 pEC50 0.06 nM EC50 J. Med. Chem. (2012) 55: 4605-4618 [PMID:22591063]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
ChEMBL Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nAChR by competition binding assay B 9.4 pKi 0.4 nM Ki ACS Med. Chem. Lett. (2014) 5: 1196-1201 [PMID:25408831]
ChEMBL Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. (2008) 16: 746-754 [PMID:17964169]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha4beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cerebral cortex homogenates after 4 hrs by liquid scintillation counting B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. (2015) 23: 5693-5701 [PMID:26233800]
ChEMBL Binding affinity to rat cortex Nicotinic acetylcholine receptor alpha4-beta2 using [3H]nicotine B 10.22 pKi 0.06 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta2 nACHR B 10.3 pKi 0.05 nM Ki J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current by two-electrode voltage clamp electrophysiological analysis B 6.7 pIC50 200 nM IC50 J. Med. Chem. (2014) 57: 836-848 [PMID:24428686]
ChEMBL Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced mean current response by two-electrode voltage clamp electrophysiology assay B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. (2015) 23: 5693-5701 [PMID:26233800]
ChEMBL Agonist activity at rat alpha4beta2 nAChR assessed as [3H]dopamine release by beta counting F 7.34 pEC50 46 nM EC50 J. Med. Chem. (2011) 54: 7588-7601 [PMID:21942635]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907591] [GtoPdb: 474465] [UniProtKB: P30926P43681]
ChEMBL Binding affinity to alpha4beta4 nAChR B 6.96 pKi 110 nM Ki J. Med. Chem. (2012) 55: 9998-10009 [PMID:23092294]
GtoPdb Binding affinity to human nicotinic acetylcholine receptor α4β2 expressed in IMR32 cells using [3H]epibatidine radioligand. - 9.96 pKi 0.11 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4889-97 [PMID:16171993]
GtoPdb In vitro affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [3H]-(−)-cytisine. - 10.4 pKi 0.04 nM Ki J. Med. Chem. (2020) 63: 2833-2853 [PMID:32026697]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907595] [GtoPdb: 465474] [UniProtKB: P09483P12392]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta4 nACHR B 6.96 pKi 110 nM Ki J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Displacement of [3H]epibatidine from rat forebrain alpha4beta4 nAChR by competition binding assay B 6.96 pKi 110 nM Ki ACS Med. Chem. Lett. (2014) 5: 1196-1201 [PMID:25408831]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 7.55 pKi 28 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs B 7.82 pKi 15 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Displacement of [3H]epibatidine from alpha7 nicotinic receptor expressed in human HEK293 cells B 6.9 pKi 125 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4749-4752 [PMID:20663668]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
ChEMBL Binding affinity to rat alpha7 nAChR expressed in Xenopus laevis oocytes B 6.52 pKi 300 nM Ki J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Binding affinity to rat alpha7 nACHR at 10 uM B 6.9 pKi 125 nM Ki J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
ChEMBL Displacement of [3H]epibatidine from rat alpha7 nAChR expressed in HEK293 cells after 4 hrs B 7.21 pKi 62 nM Ki J. Med. Chem. (2013) 56: 8404-8421 [PMID:24047231]
ChEMBL Displacement of [3H]-Epibatidine from rat alpha7 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis B 7.43 pKi 37 nM Ki J. Med. Chem. (2013) 56: 3000-3011 [PMID:23540678]
ChEMBL Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex B 7.49 pKi 32.5 nM Ki Bioorg. Med. Chem. (2008) 16: 746-754 [PMID:17964169]
ChEMBL Displacement of [125I]iodoMLA from rat cerebral cortex alpha7 nAChR at 50 nM incubated for 2 hrs by microplate scintillation assay B 7.49 pKi 32.5 nM Ki J. Med. Chem. (2012) 55: 6512-6522 [PMID:22742586]
ChEMBL Agonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay F 4.74 pEC50 18000 nM EC50 J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Agonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current by two-electrode voltage clamp electrophysiological analysis B 4.74 pEC50 18000 nM EC50 J. Med. Chem. (2014) 57: 836-848 [PMID:24428686]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptors; alpha-3/beta-4, alpha-5, beta-2 in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2221346] [GtoPdb: 472466474464] [UniProtKB: P17787P30532P30926P32297]
GtoPdb - - 7.4 pKi 39.6 nM Ki J. Med. Chem. (2020) 63: 2833-2853 [PMID:32026697]
ChEMBL Agonist activity at alpha3beta4alpha5beta2 nACHR in human SH-SY5Y cells by 86Rb+ efflux assay F 5.66 pEC50 2200 nM EC50 J. Med. Chem. (2012) 55: 812-823 [PMID:22148173]
nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor α6 subunit/Neuronal acetylcholine receptor subunit alpha-6/beta-3 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883329] [GtoPdb: 473467] [UniProtKB: P12391P43143]
ChEMBL Agonist activity at rat alpha6beta2 nAChR assessed as [3H]dopamine release by beta counting F 7.34 pEC50 46 nM EC50 J. Med. Chem. (2011) 54: 7588-7601 [PMID:21942635]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]