DHβE [Ligand Id: 4006] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL293950 (Dihydro-Beta-Erythroidine)
  • 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 α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor β2 subunit/Nicotinic acetylcholine receptor alpha-4/beta-2 in Mouse [ChEMBL: CHEMBL3301382] [GtoPdb: 474472] [UniProtKB: Q8R493Q9ERK7]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α4 subunit/Nicotinic acetylcholine receptor alpha4/beta2/alpha5 in Human [ChEMBL: CHEMBL3038461] [GtoPdb: 472466465] [UniProtKB: P17787P30532P43681]
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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 rat alpha3beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis B 4 pKi 100000 nM Ki ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
ChEMBL Activity at rat alpha3beta4 nicotinic receptor expressed in KXalpha-3-beta-4R2 cells assessed as nicotine-induced 86Rb+ efflux B 4 pIC50 100000 nM IC50 J. Nat. Prod. (2006) 69: 1514-1516 [PMID:17067175]
ChEMBL Antagonist activity at rat alpha3beta4 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay B 4 pIC50 100000 nM IC50 ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
ChEMBL Antagonist activity at rat alpha3beta4 nAChR B 4.64 pIC50 23000 nM IC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
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]cytisine from alpha4/beta2 nAChR (unknown origin) B 7.01 pKi 98 nM Ki J. Med. Chem. (2013) 56: 9673-9682 [PMID:24187998]
ChEMBL Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay B 6.39 pIC50 410 nM IC50 Bioorg. Med. Chem. (2013) 21: 2687-2694 [PMID:23561269]
ChEMBL Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. (2013) 21: 2687-2694 [PMID:23561269]
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 Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis B 6.09 pKi 820 nM Ki ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
ChEMBL Inhibition of rat membrane alpha4beta2 nAChR by [3H]cytisine binding assay B 6.85 pKi 140 nM Ki ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
ChEMBL Antagonist activity at rat alpha4beta2 nAChR B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
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 Displacement of [3H]epibatidine from rat alpha4beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis B 4 pKi 100000 nM Ki ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483]
ChEMBL Blockade of Nicotinic acetylcholine receptor alpha4-beta2 B 8.44 pIC50 3.66 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1879-1887 [PMID:15050620]
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]cytisine from alpha7 nAChR (unknown origin) B 4.98 pKi 10500 nM Ki J. Med. Chem. (2013) 56: 9673-9682 [PMID:24187998]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor β2 subunit/Nicotinic acetylcholine receptor alpha-4/beta-2 in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301382] [GtoPdb: 474472] [UniProtKB: Q8R493Q9ERK7]
ChEMBL Antagonist activity at mouse alpha4beta2 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay B 5.92 pIC50 1200 nM IC50 ACS Med. Chem. Lett. (2014) 5: 766-770 [PMID:25050162]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α4 subunit/Nicotinic acetylcholine receptor alpha4/beta2/alpha5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038461] [GtoPdb: 472466465] [UniProtKB: P17787P30532P43681]
ChEMBL Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. (2013) 21: 2687-2694 [PMID:23561269]

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]