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ChEMBL ligand: CHEMBL298517 ((1R,2R,4S)-Epibatidine, (+)-Epibatidine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
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: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
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 31:
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]