General Information of the Protein
Protein ID
PT02273
Protein Name
Vesicular acetylcholine transporter
Secondarily
Protein Name
Solute carrier family 18 member 3
Gene Name
SLC18A3
Secondarily
Gene Name
VACHT
Sequence
MESAEPAGQARAAATKLSEAVGAALQEPRRQRRLVLVIVCVALLLDNMLYMVIVPIVPDYIAHMRGGGEGPTRTPEVWEPTLPLPTPANASAYTANTSASPTAAWPAGSALRPRYPTESEDVKIGVLFASKAILQLLVNPLSGPFIDRMSYDVPLLIGLGVMFASTVLFAFAEDYATLFAARSLQGLGSAFADTSGIAMIADKYPEEPERSRALGVALAFISFGSLVAPPFGGILYEFAGKRVPFLVLAAVSLFDALLLLAVAKPFSAAARARANLPVGTPIHRLMLDPYIAVVAGALTTCNIPLAFLEPTIATWMKHTMAASEWEMGMAWLPAFVPHVLGVYLTVRLAARYPHLQWLYGALGLAVIGASSCIVPACRSFAPLVVSLCGLCFGIALVDTALLPTLAFLVDVRHVSVYGSVYAIADISYSVAYALGPIVAGHIVHSLGFEQLSLGMGLANLLYAPVLLLLRNVGLLTRSRSERDVLLDEPPQGLYDAVRLRERPVSGQDGEPRSPPGPFDACEDDYNYYYTRS
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC18 family of vesicular amine transporters
Function
Electrogenic antiporter that exchanges one cholinergic neurotransmitter, acetylcholine or choline, with two intravesicular protons across the membrane of synaptic vesicles. Uses the electrochemical proton gradient established by the V-type proton-pump ATPase to store neurotransmitters inside the vesicles prior to their release via exocytosis (PubMed:8910293, PubMed:20225888) (By similarity). Determines cholinergic vesicular quantal size at presynaptic nerve terminals in developing neuro-muscular junctions with an impact on motor neuron differentiation and innervation pattern (By similarity). Part of forebrain cholinergic system, regulates hippocampal synapse transmissions that underlie spatial memory formation (By similarity). Can transport serotonin.
    Show/Hide
Uniprot ID
Primary ID:
Q16572

Secondarily ID:
B2R7S1
    Show/Hide
HGNC ID
HGNC:10936
Subcellular Location
Cytoplasmic vesicle
Secretory vesicle
Synaptic vesicle membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL001060 , 123.7
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0200171
 Compound Info 
(+)-1''-(3-Iodo-benzyl)-4-phenyl-[1,3'']bipiperidinyl-4''-ol
   Show/Hide
C23H29IN2O
  1
1
Ki = 0.13 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0207181
 Compound Info 
(3'R,4'R)-1'-(4-Fluoro-benzyl)-4-phenyl-[1,3']bipiperidinyl-4'-ol
   Show/Hide
C23H29FN2O
  1
1
Ki = 0.22 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0045885
 Compound Info 
(1R,2R)-2-(4-Phenyl-piperidin-1-yl)-cyclohexanol
   Show/Hide
C17H25NO
  1
1
Ki = 4.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0451532
 Compound Info 
(1R,2R)-2-[4-(4-methylphenyl)piperidin-1-yl]cyclohexan-1-ol
   Show/Hide
C18H27NO
  1
1
Ki = 22.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0494571
 Compound Info 
[1-[(3S,4S)-1-benzyl-4-hydroxypiperidin-3-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H32N2O3
  1
1
Ki = 35.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0472821
 Compound Info 
[1-[(3S,4S)-1-benzyl-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H32N2O3
  1
1
Ki = 44.2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504901
 Compound Info 
[1-[(3S,4S)-1-[(4-fluorophenyl)methyl]-4-hydroxypiperidin-3-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H31FN2O3
  1
1
Ki = 48.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0490189
 Compound Info 
[1-[(3S,4S)-4-hydroxy-1-(pyridin-3-ylmethyl)piperidin-3-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C24H31N3O3
  1
1
Ki = 107 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0452454
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-1-[(4-fluorophenyl)methyl]-4-hydroxypiperidin-3-yl]piperidin-4-yl]methanone
   Show/Hide
C24H28F2N2O2
  1
1
Ki = 136 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0424933
 Compound Info 
[1-[(3S,4S)-3-hydroxy-1-(pyridin-3-ylmethyl)piperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C24H31N3O3
  1
1
Ki = 137 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504899
 Compound Info 
[1-[(3S,4S)-1-benzyl-4-hydroxypiperidin-3-yl]piperidin-4-yl]-(4-fluorophenyl)methanone
   Show/Hide
C24H29FN2O2
  1
1
Ki = 149 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504900
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-4-hydroxy-1-(pyridin-3-ylmethyl)piperidin-3-yl]piperidin-4-yl]methanone
   Show/Hide
C23H28FN3O2
  1
1
Ki = 237 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0296558
 Compound Info 
[1-[(3S,4S)-1-[(4-fluorophenyl)methyl]-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H31FN2O3
  1
1
Ki = 294 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0452453
 Compound Info 
[1-[(3S,4S)-3-hydroxy-1-(pyridine-3-carbonyl)piperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C24H29N3O4
  1
1
Ki = 372 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0424932
 Compound Info 
[1-[(3S,4S)-1-benzyl-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-fluorophenyl)methanone
   Show/Hide
C24H29FN2O2
  1
1
Ki = 401 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504905
 Compound Info 
[1-[(3S,4S)-1-benzoyl-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H30N2O4
  1
1
Ki = 555 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0505484
 Compound Info 
[1-[(3S,4S)-1-benzoyl-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-fluorophenyl)methanone
   Show/Hide
C24H27FN2O3
  1
1
Ki = 683 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0460030
 Compound Info 
[1-[(3S,4S)-4-hydroxy-1-[(4-methoxyphenyl)methyl]piperidin-3-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C26H34N2O4
  1
1
Ki = 1080 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0272134
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-1-[(4-fluorophenyl)methyl]-3-hydroxypiperidin-4-yl]piperidin-4-yl]methanone
   Show/Hide
C24H28F2N2O2
  1
1
Ki = 1360 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0389911
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-4-hydroxy-1-[(4-methoxyphenyl)methyl]piperidin-3-yl]piperidin-4-yl]methanone
   Show/Hide
C25H31FN2O3
  1
1
Ki = 1970 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0451535
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-3-hydroxy-1-(pyridin-3-ylmethyl)piperidin-4-yl]piperidin-4-yl]methanone
   Show/Hide
C23H28FN3O2
  1
1
Ki = 2030 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0389910
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-3-hydroxy-1-[(4-methoxyphenyl)methyl]piperidin-4-yl]piperidin-4-yl]methanone
   Show/Hide
C25H31FN2O3
  1
1
Ki = 3310 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0529497
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-3-hydroxy-1-(pyridine-3-carbonyl)piperidin-4-yl]piperidin-4-yl]methanone
   Show/Hide
C23H26FN3O3
  1
1
Ki = 3340 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0472822
 Compound Info 
[1-[(3S,4S)-1-(4-fluorobenzoyl)-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C25H29FN2O4
  1
1
Ki = 3460 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504904
 Compound Info 
[1-[(3S,4S)-1-(4-fluorobenzoyl)-3-hydroxypiperidin-4-yl]piperidin-4-yl]-(4-fluorophenyl)methanone
   Show/Hide
C24H26F2N2O3
  1
1
Ki = 3600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0460029
 Compound Info 
[1-[(3S,4S)-3-hydroxy-1-[(4-methoxyphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-(4-methoxyphenyl)methanone
   Show/Hide
C26H34N2O4
  1
1
Ki = 14800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0511423
 Compound Info 
(4-fluorophenyl)-[1-[(3S,4S)-3-hydroxy-1-(4-methoxybenzoyl)piperidin-4-yl]piperidin-4-yl]methanone
   Show/Hide
C25H29FN2O4
  1
1
Ki = 30900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000028 , PC-12
 Cell Line Info 
Cell Line ID: CL000868 , PC12
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0045885
 Compound Info 
(1R,2R)-2-(4-Phenyl-piperidin-1-yl)-cyclohexanol
   Show/Hide
C17H25NO
  3
1 IC50 = 20 nM
2 Ki = 2 nM
3 Ki = 15.2 nM
CP0096000
 Compound Info 
(2R,3R)-3-(4-Phenyl-piperidin-1-yl)-1,2,3,4-tetrahydro-naphthalen-2-ol
   Show/Hide
C21H25NO
  1
1 Ki = 0.055 nM
CP0200171
 Compound Info 
(+)-1''-(3-Iodo-benzyl)-4-phenyl-[1,3'']bipiperidinyl-4''-ol
   Show/Hide
C23H29IN2O
  1
1 Ki = 0.13 nM
CP0207181
 Compound Info 
(3'R,4'R)-1'-(4-Fluoro-benzyl)-4-phenyl-[1,3']bipiperidinyl-4'-ol
   Show/Hide
C23H29FN2O
  2
1 Ki = 0.22 nM
2 Ki = 0.44 nM
Clinical Information about the Protein
Target 1 ( Vesicular acetylcholine transporter (SLC18A3) )
Target Type Discontinued Target