General Information of the Protein
Protein ID
PT01929
Protein Name
Synaptic vesicular amine transporter
Secondarily
Protein Name
Monoamine transporter
Solute carrier family 18 member 2
Vesicular amine transporter 2
Gene Name
SLC18A2
Secondarily
Gene Name
SVMT
VMAT2
Sequence
MALSELALVRWLQESRRSRKLILFIVFLALLLDNMLLTVVVPIIPSYLYSIKHEKNATEIQTARPVHTASISDSFQSIFSYYDNSTMVTGNATRDLTLHQTATQHMVTNASAVPSDCPSEDKDLLNENVQVGLLFASKATVQLITNPFIGLLTNRIGYPIPIFAGFCIMFVSTIMFAFSSSYAFLLIARSLQGIGSSCSSVAGMGMLASVYTDDEERGNVMGIALGGLAMGVLVGPPFGSVLYEFVGKTAPFLVLAALVLLDGAIQLFVLQPSRVQPESQKGTPLTTLLKDPYILIAAGSICFANMGIAMLEPALPIWMMETMCSRKWQLGVAFLPASISYLIGTNIFGILAHKMGRWLCALLGMIIVGVSILCIPFAKNIYGLIAPNFGVGFAIGMVDSSMMPIMGYLVDLRHVSVYGSVYAIADVAFCMGYAIGPSAGGAIAKAIGFPWLMTIIGIIDILFAPLCFFLRSPPAKEEKMAILMDHNCPIKTKMYTQNNIQSYPIGEDEESESD
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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 cationic monoamine with two intravesicular protons across the membrane of secretory and synaptic vesicles. Uses the electrochemical proton gradient established by the V-type proton-pump ATPase to accumulate high concentrations of monoamines inside the vesicles prior to their release via exocytosis. Transports a variety of catecholamines such as dopamine, adrenaline and noradrenaline, histamine, and indolamines such as serotonin (PubMed:8643547, PubMed:23363473). Regulates the transvesicular monoaminergic gradient that determines the quantal size. Mediates somatodendritic dopamine release in hippocampal neurons, likely as part of a regulated secretory pathway that integrates retrograde synaptic signals (By similarity). Acts as a primary transporter for striatal dopamine loading ensuring impulse-dependent release of dopamine at the synaptic cleft (By similarity). Responsible for histamine and serotonin storage and subsequent corelease from mast cell granules (PubMed:8860238) (By similarity).
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Uniprot ID
Primary ID:
Q05940

Secondarily ID:
B2RC96
D3DRC4
Q15876
Q4G147
Q5VW49
Q9H3P6
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Ensembl ID
ENSG00000165646
HGNC ID
HGNC:10935
Subcellular Location
Cytoplasmic vesicle
Secretory vesicle
Synaptic vesicle membrane
Cytoplasmic vesicle
Secretory vesicle membrane
Cell projection
Axon
Cell projection
Dendrite
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0035720
(-)-reserpine
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C33H40N2O9
 5
1
IC50 = 13.2 nM
   TI
   LI
   LO
   TS
2
Kd = 8 nM
   TI
   LI
   LO
   TS
3
Ki = 5.26 nM
   TI
   LI
   LO
   TS
4
Ki = 410 nM
   TI
   LI
   LO
   TS
5
Ki = 630 nM
   TI
   LI
   LO
   TS
CP0542828
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-phenylpiperidine-3-carboxylate
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C24H27N3O4
 4
1
IC50 = 19.7 nM
   TI
   LI
   LO
   TS
2
Ki = 70 nM
   TI
   LI
   LO
   TS
3
Ki = 287 nM
   TI
   LI
   LO
   TS
4
Ki > 7700 nM
   TI
   LI
   LO
   TS
CP0485162
9,10-dimethoxy-3-(2-methylpropyl)-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-ol
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C19H29NO3
 5
1
IC50 = 28.1 nM
   TI
   LI
   LO
   TS
2
Kd = 71 nM
   TI
   LI
   LO
   TS
3
Ki = 70 nM
   TI
   LI
   LO
   TS
4
Ki = 152 nM
   TI
   LI
   LO
   TS
5
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0262735
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-fluorophenyl)piperidine-3-carboxylate
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C24H26FN3O4
 4
1
IC50 = 39.4 nM
   TI
   LI
   LO
   TS
2
Ki = 74 nM
   TI
   LI
   LO
   TS
3
Ki = 161 nM
   TI
   LI
   LO
   TS
4
Ki > 7400 nM
   TI
   LI
   LO
   TS
CP0391815
ethyl (3S,4R)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-fluorophenyl)piperidine-3-carboxylate
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C24H26FN3O4
 4
1
IC50 = 85.5 nM
   TI
   LI
   LO
   TS
2
Ki = 176 nM
   TI
   LI
   LO
   TS
3
Ki = 750 nM
   TI
   LI
   LO
   TS
4
Ki = 1150 nM
   TI
   LI
   LO
   TS
CP0370076
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-thiophen-2-ylpiperidine-3-carboxylate
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C22H25N3O4S
 4
1
IC50 = 101 nM
   TI
   LI
   LO
   TS
2
Ki = 450 nM
   TI
   LI
   LO
   TS
3
Ki = 900 nM
   TI
   LI
   LO
   TS
4
Ki = 6160 nM
   TI
   LI
   LO
   TS
CP0368363
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperidine-3-carboxylate
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C25H26F3N3O4
 4
1
IC50 = 125 nM
   TI
   LI
   LO
   TS
2
Ki = 350 nM
   TI
   LI
   LO
   TS
3
Ki = 990 nM
   TI
   LI
   LO
   TS
4
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0329619
ethyl (3S,4S)-4-(2,3-dihydro-1,4-benzodioxin-5-yl)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]piperidine-3-carboxylate
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C26H29N3O6
 4
1
IC50 = 142 nM
   TI
   LI
   LO
   TS
2
Ki = 652 nM
   TI
   LI
   LO
   TS
3
Ki = 700 nM
   TI
   LI
   LO
   TS
4
Ki > 7900 nM
   TI
   LI
   LO
   TS
CP0391814
2-ethyl-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-ol
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C21H33NO3
 4
1
IC50 = 154 nM
   TI
   LI
   LO
   TS
2
Ki = 64 nM
   TI
   LI
   LO
   TS
3
Ki = 83 nM
   TI
   LI
   LO
   TS
4
Ki = 1932 nM
   TI
   LI
   LO
   TS
CP0055933
3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione
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C22H22FN3O3
 4
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
2
Ki = 77 nM
   TI
   LI
   LO
   TS
3
Ki = 353 nM
   TI
   LI
   LO
   TS
4
Ki = 1190 nM
   TI
   LI
   LO
   TS
CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
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C10H12N2O
 3
1
IC50 = 1430 nM
   TI
   LI
   LO
   TS
2
Ki = 2290 nM
   TI
   LI
   LO
   TS
3
Ki = 7690 nM
   TI
   LI
   LO
   TS
CP0391812
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-methylphenyl)piperidine-3-carboxylate
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C25H29N3O4
 4
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
2
Ki = 452 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
4
Ki > 9100 nM
   TI
   LI
   LO
   TS
CP0472846
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-[4-(trifluoromethyl)phenyl]piperidine-3-carboxylate
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C25H26F3N3O4
 3
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
2
Ki = 720 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0468811
(R)Methyl-(1-methyl-2-phenyl-ethyl)-amine
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C10H15N
 3
1
IC50 = 3620 nM
   TI
   LI
   LO
   TS
2
Ki = 6400 nM
   TI
   LI
   LO
   TS
3
Ki = 24500 nM
   TI
   LI
   LO
   TS
CP0011881
(-)-lobeline
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C22H27NO2
 4
1
IC50 = 4200 nM
   TI
   LI
   LO
   TS
2
Ki = 1840 nM
   TI
   LI
   LO
   TS
3
Ki = 1950 nM
   TI
   LI
   LO
   TS
4
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0329617
ethyl (3S,4S)-4-[4-(dimethylamino)phenyl]-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]piperidine-3-carboxylate
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C26H32N4O4
 3
1
IC50 = 5800 nM
   TI
   LI
   LO
   TS
2
Ki = 1960 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0329618
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-ethoxycarbonylphenyl)piperidine-3-carboxylate
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C27H31N3O6
 3
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
2
Ki = 1660 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0417151
ethyl (3S,4S)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-phenylphenyl)piperidine-3-carboxylate
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C30H31N3O4
 3
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
2
Ki = 3770 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0115748
ethyl 1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-fluorophenyl)piperidine-3-carboxylate
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C24H26FN3O4
 2
1
Kd = 93 nM
   TI
   LI
   LO
   TS
2
Ki = 290 nM
   TI
   LI
   LO
   TS
CP0391813
1,2-ditritioethyl (3R,4R)-1-[2-(2,4-dioxo-1H-quinazolin-3-yl)ethyl]-4-(4-fluorophenyl)piperidine-3-carboxylate
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C24H26FN3O4
 1
1
Kd = 93 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Synaptic vesicle amine transporter (SLC18A2) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Hypertension [ICD-11: BA00-BA04]
2 Hyperkinetic movement disorder [ICD-11: 6B60.8]
3 Movement disorder [ICD-11: 8A07-8A0Z]
4 Tardive dyskinesia [ICD-11: 8A02.10]
5 Substance use disorder [ICD-11: 6C4Z]
Approved Drug(s) 3 Approved Drugs  3
1 Reserpine Approved
Hypertension
2 Tetrabenazine Approved
Hyperkinetic movement disorder
3 Ingrezza Phase 4
Tardive dyskinesia
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 NBI-98854 Phase 3
Movement disorder
2 Lobeline Phase 2
Substance use disorder