choline [Ligand Id: 4551] 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: CHEMBL920 (Choline)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
There should be some charts here, you may need to enable JavaScript!
  • 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 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!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
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
CHT/Choline transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3013] [GtoPdb: 914] [UniProtKB: Q8BGY9]
ChEMBL In vitro ability to inhibit the transport of [3H]choline in to high affinity choline transport system HAChT B 5.8 pIC50 1600 nM IC50 J. Med. Chem. (1986) 29: 376-380 [PMID:3950917]
CT1/Creatine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3814] [GtoPdb: 934] [UniProtKB: P28570]
ChEMBL Inhibition of [3H]-choline brain uptake was determined by in situ brain perfusion studies in male rats B 4.38 pKi 42000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 3085-3092 [PMID:15149650]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
ChEMBL Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand B 4.38 pKi 42000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
ChEMBL Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 4.74 pKi 18000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 4.43 pKi 37000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
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 Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand B 4.32 pKi 48000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
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 Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 4.43 pKi 37000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
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 Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand B 4.47 pKi 34000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes F 4.26 pIC50 55000 nM IC50 Biochem. Biophys. Res. Commun. (2002) 296: 644-650 [PMID:12176030]

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]