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: 464, 474] [UniProtKB: P04757, P12392] There should be some charts here, you may need to enable JavaScript!
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4] There should be some charts here, you may need to enable JavaScript!

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: 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]