varenicline [Ligand Id: 5459] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1396 (Chantix, CP-526,555, CP-526555, Varenicline) |
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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: 462, 475, 471, 476] [UniProtKB: P02708, P07510, P11230, Q07001] | ||||||||
| 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: 463, 472] [UniProtKB: P12389, P12390] | ||||||||
| 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: 463, 474] [UniProtKB: P12389, P12392] | ||||||||
| 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: 464, 472] [UniProtKB: P32297, P17787] | ||||||||
| 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: 464, 472] [UniProtKB: P04757, P12390] | ||||||||
| 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: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| 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: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
| 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: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| 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: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| 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: 474, 465] [UniProtKB: P30926, P43681] | ||||||||
| 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: 465, 474] [UniProtKB: P09483, P12392] | ||||||||
| 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: 472, 466, 474, 464] [UniProtKB: P17787, P30532, P30926, P32297] | ||||||||
| 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: 473, 467] [UniProtKB: P12391, P43143] | ||||||||
| 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 33:
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]
