choline [Ligand Id: 4551] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL920 (Choline)
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  • 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]
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  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
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  • 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 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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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
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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 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]