epibatidine [Ligand Id: 5348] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL298517 ((1R,2R,4S)-Epibatidine, (+)-Epibatidine)
  • 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 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
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 Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates B 9.42 pKi 0.38 nM Ki J. Med. Chem. (2005) 48: 5123-5130 [PMID:16078832]
ChEMBL Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor expressed in IMR32 cell B 6.15 pEC50 700 nM EC50 J. Med. Chem. (2005) 48: 5123-5130 [PMID:16078832]
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 alpha4beta2 nAChR (unknown origin) B 10.35 pKi 0.04 nM Ki Eur. J. Med. Chem. (2015) 103: 429-437 [PMID:26383127]
ChEMBL Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR B 10.59 pKi 0.03 nM Ki J. Med. Chem. (2007) 50: 6383-6391 [PMID:17994682]
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 9.8 pKi 0.16 nM Ki J. Med. Chem. (2002) 45: 3041-3047 [PMID:12086489]
ChEMBL Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 15 B 10.26 pKi 0.06 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1889-1896 [PMID:15050621]
ChEMBL Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates B 10.3 pKi 0.05 nM Ki J. Med. Chem. (2005) 48: 5123-5130 [PMID:16078832]
ChEMBL Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 14 B 10.35 pKi 0.04 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1889-1896 [PMID:15050621]
ChEMBL Non-specific binding in presence of 300 uM nicotine at nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex membranes B 10.35 pKi 0.04 nM Ki J. Med. Chem. (2001) 44: 2229-2237 [PMID:11405659]
ChEMBL Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cerebral cortex after 4 hrs by scintillation counting B 10.59 pKi 0.03 nM Ki J. Nat. Prod. (2010) 73: 306-312 [PMID:20038125]
ChEMBL Displacement of [3H]epibatidine from alpha-4-beta-2 nACHR in rat cerebral cortex B 10.59 pKi 0.03 nM Ki J. Med. Chem. (2006) 49: 3244-3250 [PMID:16722642]
ChEMBL Inhibition of [3H]epibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex B 10.59 pKi 0.03 nM Ki J. Med. Chem. (2001) 44: 2229-2237 [PMID:11405659]
ChEMBL Inhibition of alpha beta[3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cerebral cortex B 10.7 pKi 0.02 nM Ki J. Med. Chem. (2004) 47: 4588-4594 [PMID:15317468]
ChEMBL Displacement of [3H]Nicotine from alpha4beta2 nAChR in rat cortical membranes B 10.72 pKi 0.02 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 5493-5497 [PMID:16934977]
ChEMBL Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 16 B 10.74 pKi 0.02 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1889-1896 [PMID:15050621]
ChEMBL Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cerebral cortex after 4 hrs by scintillation counting B 10.74 pKi 0.02 nM Ki J. Nat. Prod. (2010) 73: 306-312 [PMID:20038125]
ChEMBL In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 F 8.89 pEC50 1.3 nM EC50 J. Med. Chem. (2002) 45: 3041-3047 [PMID:12086489]
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 Agonist activity at human recombinant alpha7 nAChR expressed in rat GH3 cells by calcium influx assay F 7.4 pEC50 39.81 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 1287-1291 [PMID:19208472]
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 Displacement of [125I-alpha]-Bungarotoxin from alpha-7 nAChR in rat hippocampal membranes B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 5493-5497 [PMID:16934977]
Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4]
ChEMBL Displacement of [3HIMI from nicotinic acetylcholine receptor in Musca domestica (house fly) head membranes incubated for 60 min by liquid scintillation counting method B 5.55 pIC50 2790 nM IC50 Biosci. Biotechnol. Biochem. (2003) 67: 980-988 [PMID:12834274]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]