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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
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: 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]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat [ChEMBL: CHEMBL1907595] [GtoPdb: 465474] [UniProtKB: P09483P12392]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483]
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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
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: 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 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]