cytisine [Ligand Id: 5347] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL497939 (6039 Sopharma, Baptitoxine, Cytisine, Cytisinicline, Cytiton, NSC-407282, Sophorine, Tabex, Ulexine)
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  • 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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  • Acetylcholine receptor protein alpha chain in Torpedo californica [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
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  • Acetylcholine receptor protein delta chain in Torpedo californica [ChEMBL: CHEMBL3916] [UniProtKB: P02718]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
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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 β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human [ChEMBL: CHEMBL2109234] [GtoPdb: 472464] [UniProtKB: P17787P32297]
  • 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 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 alpha 5 subunit in Musca domestica [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine receptor in Torpedo californica (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096975] [UniProtKB: P02710P02712P02714P02718]
ChEMBL Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha1 beta gamma delta of electroplax B 6.6 pKi 250 nM Ki J Med Chem (2005) 48: 3474-3477 [PMID:15887955]
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 human Nicotinic acetylcholine receptor alpha-1-beta-gamma-delta expressed in HEK 293 cells using [3H]alpha-bungarotoxin B 6.6 pKi 250 nM Ki Bioorg Med Chem Lett (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors F 7.96 pEC50 11 nM EC50 Bioorg Med Chem Lett (2005) 15: 1221-1224 [PMID:15686946]
Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
ChEMBL Displacement of [3H]alpha-BGT from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method B 5.45 pIC50 3530 nM IC50 J Pestic Sci (1995) 20: 49-56
Acetylcholine receptor protein delta chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3916] [UniProtKB: P02718]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype TE671 (muscle) B 4 pEC50 100000 nM EC50 J Med Chem (1997) 40: 4169-4194 [PMID:9435889]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
ChEMBL Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand B 8.6 pKi 2.5 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic) B 5 pEC50 10000 nM EC50 J Med Chem (1997) 40: 4169-4194 [PMID:9435889]
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 Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]epibatidine from rat alpha-2-beta-2 nACHR expressed in human HEK293 cells B 8.97 pKi 1.07 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
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 alpha-2-beta-4 nACHR expressed in human HEK293 cells B 8.27 pKi 5.41 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2109234] [GtoPdb: 472464] [UniProtKB: P17787P32297]
ChEMBL Effective concentration against Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes B 4.17 pEC50 67000 nM EC50 J Med Chem (2005) 48: 4705-4745 [PMID:16033252]
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 alpha-3-beta-2 nACHR expressed in human HEK293 cells B 7.43 pKi 37.2 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 7.43 pKi 37 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
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 Displacement of [3H]epibatidine from human alpha3beta4 nAChR in IMR32 cells B 5.81 pKi 1560 nM Ki Bioorg Med Chem Lett (2008) 18: 2316-2319 [PMID:18356044]
ChEMBL Inhibition of [3H]epibatidine binding to nicotinic acetylcholine receptor alpha3-beta4 of human IMR32 cells B 6.08 pKi 840 nM Ki J Med Chem (2005) 48: 3474-3477 [PMID:15887955]
ChEMBL Binding affinity to human Nicotinic acetylcholine receptor alpha3-beta4 expressed in IMR32 cells using [3H]epibatidine B 6.08 pKi 840 nM Ki Bioorg Med Chem Lett (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Inhibition of [3H]epibatidine binding to nicotinic acetylcholine receptor alpha3-beta4 of IMR32 cells B 6.08 pKi 840 nM Ki Bioorg Med Chem Lett (2005) 15: 2974-2979 [PMID:15908213]
ChEMBL Displacement of [3H]epibatidine from human recombinant alpha-3-beta-4 nAChR in HEK293 cells by SPA assay B 6.28 pKi 525 nM Ki Bioorg Med Chem Lett (2006) 16: 5493-5497 [PMID:16934977]
ChEMBL Partial agonist activity at alpha3beta4 nAChR (unknown origin) B 6.32 pKi 480 nM Ki J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK cells B 6.55 pKi 280 nM Ki J Nat Prod (2013) 76: 727-731 [PMID:23461628]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) B 4.59 pEC50 26000 nM EC50 J Med Chem (1997) 40: 4169-4194 [PMID:9435889]
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 human HEK293 cells B 6.66 pKi 217 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand B 6.68 pKi 210 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs B 6.69 pKi 203 nM Ki J Med Chem (2010) 53: 8187-8191 [PMID:20979364]
ChEMBL Effective concentration in KXalpha-3-beta-4R2 cells expressing rat nicotinic acetylcholine receptor alpha3-beta4 subunits F 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (2005) 15: 1221-1224 [PMID:15686946]
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 Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assay B 8.59 pKi 2.59 nM Ki Bioorg Med Chem Lett (2006) 16: 5493-5497 [PMID:16934977]
ChEMBL Partial agonist activity at alpha4beta2 nAChR (unknown origin) B 8.7 pKi 2 nM Ki J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Displacement of [3H]cytisine from human alpha4beta2 nAChR by Cheng-Prusoff equation analysis B 9.55 pKi 0.28 nM Ki Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 in human HEK293 cells using [3H]- nicotine as radioligand B 9.64 pKi 0.23 nM Ki Bioorg Med Chem Lett (2005) 15: 2974-2979 [PMID:15908213]
ChEMBL Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotine B 9.64 pKi 0.23 nM Ki Bioorg Med Chem Lett (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Inactivation of alpha4beta2* nAChR low affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 4.55 pIC50 28000 nM IC50 J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Inactivation of alpha4beta2* nAChR high affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 7.3 pIC50 50 nM IC50 J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2 B 4.42 pEC50 38000 nM EC50 J Med Chem (1997) 40: 4169-4194 [PMID:9435889]
ChEMBL Activation of alpha4beta2* nAChR high affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 5.7 pEC50 2000 nM EC50 J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits F 9.38 pEC50 0.42 nM EC50 Bioorg Med Chem Lett (2005) 15: 1221-1224 [PMID:15686946]
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 in vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 B 8.38 pKi 4.2 nM Ki J Med Chem (2002) 45: 3041-3047 [PMID:12086489]
ChEMBL In vitro binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]cytisine in rat brain B 8.56 pKi 2.78 nM Ki J Med Chem (2001) 44: 4704-4715 [PMID:11741488]
ChEMBL Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex B 8.68 pKi 2.1 nM Ki J Nat Prod (2013) 76: 727-731 [PMID:23461628]
ChEMBL Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nACHR B 8.72 pKi 1.92 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs B 8.82 pKi 1.53 nM Ki J Med Chem (2010) 53: 8187-8191 [PMID:20979364]
ChEMBL Displacement of [3H]epibatidine from rat alpha-4-beta-2 nACHR expressed in human HEK293 cells B 8.82 pKi 1.51 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 8.82 pKi 1.5 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]cytisine from rat alpha4beta2 nAChR in rat brain cell membrane B 8.97 pKi 1.06 nM Ki Bioorg Med Chem Lett (2010) 20: 6667-6670 [PMID:20880707]
ChEMBL Binding affinity to rat alpha4beta2 nAChR B 9 pKi 1 nM Ki J Med Chem (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates B 9.32 pKi 0.48 nM Ki J Med Chem (2009) 52: 4345-4357 [PMID:19548687]
ChEMBL Displacement of [3H]nicotine from alpha4beta2 nAChR in Sprague-Dawley rat brain membrane B 9.37 pKi 0.43 nM Ki Bioorg Med Chem Lett (2008) 18: 2316-2319 [PMID:18356044]
ChEMBL Displacement of [3H]nicotine from rat alpha4beta2 nAChR by liquid scintillation counting B 9.4 pKi 0.4 nM Ki Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nAChR in rat cortical membrane B 9.4 pKi 0.4 nM Ki Bioorg Med Chem (2010) 18: 4498-4508 [PMID:20478710]
ChEMBL Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates B 9.47 pKi 0.34 nM Ki J Med Chem (2009) 52: 4345-4357 [PMID:19548687]
ChEMBL Inhibition of [3H]-nicotine binding to nicotinic acetylcholine receptor alpha4-beta2 in rat cortex B 9.77 pKi 0.17 nM Ki Bioorg Med Chem Lett (2005) 15: 2974-2979 [PMID:15908213]
ChEMBL Inhibition of [3H]nicotine binding to nicotinic acetylcholine receptor alpha4-beta2 of rat cortex B 9.77 pKi 0.17 nM Ki J Med Chem (2005) 48: 3474-3477 [PMID:15887955]
ChEMBL In vitro binding affinity towards (alpha-4)2(beta-2)3 neuronal nicotinic acetylcholine receptor in P2 membrane fractions of rat forebrain B 9.91 pKi 0.12 nM Ki J Med Chem (2003) 46: 2031-2048 [PMID:12747776]
ChEMBL Displacement of [3H]epibatidine from Sprague-Dawley rat brain alpha4beta2 nAChR after 90 mins by liquid scintillation counting analysis B 9.91 pKi 0.12 nM Ki Bioorg Med Chem (2013) 21: 7309-7329 [PMID:24145137]
ChEMBL Displacement of [3H]-epibatidine from rat forebrain alpha4beta2 nAChR B 9.91 pKi 0.12 nM Ki Bioorg Med Chem (2013) 21: 7283-7308 [PMID:24156938]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta2 nAChR B 7.16 pIC50 69.18 nM IC50 Bioorg Med Chem Lett (2010) 20: 3683-3687 [PMID:20493692]
ChEMBL In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 F 8.06 pEC50 8.8 nM EC50 J Med Chem (2002) 45: 3041-3047 [PMID:12086489]
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 Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand B 8.66 pKi 2.2 nM Ki Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]epibatidine from rat alpha-4-beta-4 nACHR expressed in human HEK293 cells B 8.68 pKi 2.1 nM Ki J Med Chem (2006) 49: 2673-2676 [PMID:16640326]
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 Partial agonist activity at alpha7 nAChR (unknown origin) B 5.23 pKi 5890 nM Ki J Med Chem (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Inhibition of [3H]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha7 of IMR32 cells B 5.38 pKi 4200 nM Ki Bioorg Med Chem Lett (2005) 15: 2974-2979 [PMID:15908213]
ChEMBL Binding affinity to human Nicotinic acetylcholine receptor alpha7 expressed in IMR32 cells using [3H]alpha-bungarotoxin B 5.85 pKi 1420 nM Ki Bioorg Med Chem Lett (2005) 15: 4889-4897 [PMID:16171993]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha7 B 4.15 pEC50 71000 nM EC50 J Med Chem (1997) 40: 4169-4194 [PMID:9435889]
ChEMBL Effective concentration against Nicotinic acetylcholine receptor alpha 7 expressed in xenopus oocytes B 4.15 pEC50 71000 nM EC50 J Med Chem (2005) 48: 4705-4745 [PMID:16033252]
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 B 5.1 pKi 8000 nM Ki J Med Chem (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Displacement of [125I]alpha-bungarotoxin from rat alpha7 nAChR in GH4C1 cells B 5.24 pKi 5820 nM Ki Bioorg Med Chem Lett (2008) 18: 2316-2319 [PMID:18356044]
ChEMBL Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha-7 subunit in rat GH4C1 cells B 5.38 pKi 4200 nM Ki J Med Chem (2005) 48: 3474-3477 [PMID:15887955]
ChEMBL Displacement of [3H]MLA from rat alpha7 nAChR by liquid scintillation counting B 5.77 pKi 1700 nM Ki Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Displacement of [125I]alpha-Bungarotoxin from alpha7 nAchR in rat brain cell membrane B 6 pKi 1000 nM Ki Bioorg Med Chem Lett (2010) 20: 6667-6670 [PMID:20880707]
ChEMBL Displacement of [125I]alpha-bungarotoxin from alpha7 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates B 6.48 pKi 331 nM Ki J Med Chem (2009) 52: 4345-4357 [PMID:19548687]
ChEMBL Displacement of [125I]alpha-Bungarotoxin from alpha7 nAChR in rat cortical membrane B 6.52 pKi 300 nM Ki Bioorg Med Chem (2010) 18: 4498-4508 [PMID:20478710]
ChEMBL Displacement of [3H]methyllycaconitine from Sprague-Dawley rat brain alpha7 nAChR after 120 mins by liquid scintillation counting analysis B 6.58 pKi 261 nM Ki Bioorg Med Chem (2013) 21: 7309-7329 [PMID:24145137]
ChEMBL Displacement of [3H]methyllycaconitine from rat forebrain alpha7 nAChR B 6.6 pKi 250 nM Ki Bioorg Med Chem (2013) 21: 7283-7308 [PMID:24156938]
ChEMBL Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR from rat hippocampus B 6.64 pKi 230 nM Ki J Nat Prod (2013) 76: 727-731 [PMID:23461628]
ChEMBL In vitro binding affinity towards Nicotinic acetylcholine receptor alpha7 using [125I]-alpha-Bungarotoxin in rat brain B 9.05 pKi 0.9 nM Ki J Med Chem (2001) 44: 4704-4715 [PMID:11741488]
Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4]
ChEMBL Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting B 5.91 pKi 1230 nM Ki J Pestic Sci (1992) 17: 231-236

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]