4OH-GTS-21 [Ligand Id: 11385] 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: CHEMBL1162395
  • Acetylcholine-binding protein in Lymnaea stagnalis [ChEMBL: CHEMBL6084] [UniProtKB: P58154]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
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 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!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine-binding protein in Lymnaea stagnalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6084] [UniProtKB: P58154]
ChEMBL Displacement of [3H]-epibatidine from Lymnaea stagnalis N-terminal FLAG-tagged AChBP expressed in HEK293 cells after 2 hrs by liquid scintillation counting B 9.4 pKd 0.4 nM Kd Eur. J. Med. Chem. (2011) 46: 5625-5635 [PMID:21986237]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
ChEMBL Displacement of [3H]-epibatidine from alpha3beta4 nAChR in human SH-SY5Y cellular membranes after 2 hrs by liquid scintillation counting B 6.01 pKi 970 nM Ki Eur. J. Med. Chem. (2011) 46: 5625-5635 [PMID:21986237]
ChEMBL Displacement of [3H]epibatidine from human alpha3beta4 nAchR expressed in SH-SY5Y cells B 6.01 pKi 970 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 1179-1186 [PMID:22177081]
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]epibatidine from human alpha4beta2 nAchR expressed in SH-EP1 cells B 7.72 pKi 19 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 1179-1186 [PMID:22177081]
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]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs B 1.16 pKi 1.16 uM pKi Eur. J. Med. Chem. (2010) 45: 2433-2446 [PMID:20236734]
ChEMBL Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs B 7.15 pKi 70 nM Ki Eur. J. Med. Chem. (2010) 45: 2433-2446 [PMID:20236734]
ChEMBL Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortical membranes after 2 hrs by liquid scintillation counting B 7.72 pKi 19 nM Ki Eur. J. Med. Chem. (2011) 46: 5625-5635 [PMID:21986237]
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 [125I]alpha-bungarotoxin from alpha7 nAChR B 7.64 pKd 23 nM Kd J. Med. Chem. (2008) 51: 6293-6302 [PMID:18826295]
ChEMBL Agonist activity at human cloned wild-type alpha7 nAChR expressed in Xenopus laevis oocytes assessed as channel opening by voltage clamp electrophysiology F 5.52 pEC50 3000 nM EC50 J. Med. Chem. (2008) 51: 6293-6302 [PMID:18826295]
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 alpha7 nAChR in rat brain membrane after 3 hrs B 0.62 pKi 0.62 uM pKi Eur. J. Med. Chem. (2010) 45: 2433-2446 [PMID:20236734]
ChEMBL Displacement of [3H]-methyllycaconitine from alpha7 nAChR in rat hippocampal membranes after 2 hrs by liquid scintillation counting B 6.38 pKi 420 nM Ki Eur. J. Med. Chem. (2011) 46: 5625-5635 [PMID:21986237]
GtoPdb Displacement of [3H]-methyllycaconitine from rat α7 nAChR in hippocampal membranes by liquid scintillation counting - 6.38 pKi 420 nM Ki Eur J Med Chem (2011) 46: 5625-35 [PMID:21986237]
ChEMBL Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs B 6.62 pKi 240 nM Ki Eur. J. Med. Chem. (2010) 45: 2433-2446 [PMID:20236734]
ChEMBL Agonist activity at rat recombinant alpha7 nAChR expressed in GH4C1 cells by patch clamp technique F 5.8 pEC50 1600 nM EC50 Eur. J. Med. Chem. (2011) 46: 5625-5635 [PMID:21986237]

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]