General Information of the Protein
Protein ID
PT00871
Protein Name
Sodium-dependent serotonin transporter
Secondarily
Protein Name
5HT transporter
Solute carrier family 6 member 4
Gene Name
SLC6A4
Secondarily
Gene Name
HTT
SERT
Sequence
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTRHSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLPYTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIMAWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIHRSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGATLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQDALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPASTFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVTLTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRICWVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIITPGTFKERIIKSITPETPTEIPCGDIRLNAV
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC06 neurotransmitter transporter family
Function
Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:27756841, PubMed:34851672, PubMed:21730057, PubMed:10407194, PubMed:27049939, PubMed:12869649). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cortex, acts in glutamatergic neurons to control serotonin uptake and its trophic functions accounting for proper spatial organization of cortical neurons and elaboration of sensory circuits. In the mature cortex, acts primarily in brainstem raphe neurons to mediate serotonin uptake from the synaptic cleft back into the pre-synaptic terminal thus terminating serotonin signaling at the synapse (By similarity). Modulates mucosal serotonin levels in the gastrointestinal tract through uptake and clearance of serotonin in enterocytes. Required for enteric neurogenesis and gastrointestinal reflexes (By similarity). Regulates blood serotonin levels by ensuring rapid high affinity uptake of serotonin from plasma to platelets, where it is further stored in dense granules via vesicular monoamine transporters and then released upon stimulation (PubMed:17506858, PubMed:18317590). Mechanistically, the transport cycle starts with an outward-open conformation having Na1(+) and Cl(-) sites occupied. The binding of a second extracellular Na2(+) ion and serotonin substrate leads to structural changes to outward-occluded to inward-occluded to inward-open, where the Na2(+) ion and serotonin are released into the cytosol. Binding of intracellular K(+) ion induces conformational transitions to inward-occluded to outward-open and completes the cycle by releasing K(+) possibly together with a proton bound to Asp-98 into the extracellular compartment. Na1(+) and Cl(-) ions remain bound throughout the transport cycle (PubMed:27756841, PubMed:34851672, PubMed:21730057, PubMed:10407194, PubMed:27049939, PubMed:12869649). Additionally, displays serotonin-induced channel-like conductance for monovalent cations, mainly Na(+) ions. The channel activity is uncoupled from the transport cycle and may contribute to the membrane resting potential or excitability (By similarity).
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Uniprot ID
Primary ID:
P31645

Secondarily ID:
Q5EE02
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Ensembl ID
ENSG00000108576
HGNC ID
HGNC:11050
Subcellular Location
Cell membrane
Endomembrane system
Endosome membrane
Synapse
Cell junction
Focal adhesion
Cell projection
Neuron projection
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: CL000109 , COS-1
Compound ID Compound Name Compound Formula
CP0567099
4-(dimethylamino)-1-[1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3H-2-benzofuran-5-yl]butan-1-one
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C25H33FN2O2
 1
1
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0041286
(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
   Show/Hide
C20H21FN2O
 1
1
IC50 = 2.1 nM
   TI
   LI
   LO
   TS
CP0389750
3-[3-(4-fluorophenyl)-1H-benzo[e][2]benzofuran-3-yl]-N,N-dimethylpropan-1-amine
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C23H24FNO
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0041749
1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
   Show/Hide
C20H21FN2O
 1
1
IC50 = 6.7 nM
   TI
   LI
   LO
   TS
CP0457713
3-[3-(4-fluorophenyl)-1H-benzo[f][2]benzofuran-3-yl]-N,N-dimethylpropan-1-amine
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C23H24FNO
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0564933
3-[1-(4-fluorophenyl)-3H-benzo[g][2]benzofuran-1-yl]-N,N-dimethylpropan-1-amine
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C23H24FNO
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0564932
3-[1-(3,4-dichlorophenyl)-3H-2-benzofuran-1-yl]-N,N-dimethylpropan-1-amine
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C19H21Cl2NO
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0518453
R-citalopram
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C20H21FN2O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0452894
methyl (2S,3S)-8-methyl-3-(4-thiophen-3-ylphenyl)-8-azabicyclo[3.2.1]octane-2-carboxylate
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C20H23NO2S
 1
1
Ki = 0.58 nM
   TI
   LI
   LO
   TS
CP0374067
1-[3beta-(4-Chloro-phenyl)tropane-2beta-carbonyl-oxy]-6-[4-(3beta-{4-chloro-phenyl}tropane-2beta-carbonyl-oxy-methyl)-(1,2,3)triazol-1-yl]hexane
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C39H49Cl2N5O4
 1
1
Ki = 0.86 nM
   TI
   LI
   LO
   TS
CP0452254
1-[3beta-(4-Chloro-phenyl)tropane-2beta-carbonyl-oxy]-7-[4-(3beta-{4-chloro-phenyl}tropane-2beta-carbonyl-oxy-methyl)-(1,2,3)triazol-1-yl]heptane
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C40H51Cl2N5O4
 1
1
Ki = 3.5 nM
   TI
   LI
   LO
   TS
CP0463007
(1S,2S,3S,5R)-methyl 3-(4-iodophenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate
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C16H20INO2
 2
1
Ki = 4 nM
   TI
   LI
   LO
   TS
2
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0845401
(2S,3S)-3-(4-Iodo-phenyl)-2-methoxycarbonyl-8-methyl-8-azonia-bicyclo[3.2.1]octane
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C16H20INO2
 1
1
Ki = 4.2 nM
   TI
   LI
   LO
   TS
CP0374068
1-[3beta-(4-Chlorophenyl)tropane-2beta-carbonyl-oxy]-5-[(1,2,3)triazol-1-yl]pentane
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C22H29ClN4O2
 1
1
Ki = 20 nM
   TI
   LI
   LO
   TS
CP0374069
methyl (2S,3S)-3-(4-chlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
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C16H20ClNO2
 1
1
Ki = 21 nM
   TI
   LI
   LO
   TS
CP0452256
1-[3beta-(4-Chloro-phenyl)tropane-2beta-carbonyl-oxy]-2-[4-(3beta-{4-chloro-phenyl}tropane-2beta-carbonyl-oxy-methyl)-(1,2,3)triazol-1-yl]ethane
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C35H41Cl2N5O4
 1
1
Ki = 27 nM
   TI
   LI
   LO
   TS
CP0452255
1-[3beta-(4-Thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]-2-[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylaminomethylbenzene-4-yl]ethane
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C47H52N4O2S2
 1
1
Ki = 62 nM
   TI
   LI
   LO
   TS
CP0374071
1-[3beta-(4-Chlorophenyl)tropane-2beta-carbonyl-amino]-2-[3beta-(4-chlorophenyl)tropane-2beta-carbonylaminomethylbenzene-4-yl]ethane
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C39H46Cl2N4O2
 1
1
Ki = 65 nM
   TI
   LI
   LO
   TS
CP0374070
1,4-Di[3-(4-thiophene-3-yl-phenyl)tropane-2-carbonylaminomethyl]benzene
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C46H50N4O2S2
 1
1
Ki = 160 nM
   TI
   LI
   LO
   TS
CP0405661
ethyl 4-(3,4-dichlorophenyl)-1,2,3,6-tetrahydropyridine-5-carboxylate
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C14H15Cl2NO2
 1
1
Ki = 217 nM
   TI
   LI
   LO
   TS
CP0400422
1,10-Di[3beta-(4-thiophene-3-yl-phenyl)tropane-2bcarbonyl-amino]decane
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C48H62N4O2S2
 1
1
Ki = 250 nM
   TI
   LI
   LO
   TS
CP0439052
1,4-Di[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]benzene
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C44H46N4O2S2
 1
1
Ki = 270 nM
   TI
   LI
   LO
   TS
CP0425668
(3S,4S)-methyl 4-(4-iodophenyl)-1-methylpiperidine-3-carboxylate
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C14H18INO2
 1
1
Ki = 287 nM
   TI
   LI
   LO
   TS
CP0417950
1-[3beta-(4-Thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]-2-[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylaminobenzene-4-yl]ethane
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C46H50N4O2S2
 1
1
Ki = 340 nM
   TI
   LI
   LO
   TS
CP0510902
ethyl 4-naphthalen-2-yl-1,2,3,6-tetrahydropyridine-5-carboxylate
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C18H19NO2
 1
1
Ki = 440 nM
   TI
   LI
   LO
   TS
CP0452897
1,8-Di[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]octane
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C46H58N4O2S2
 1
1
Ki = 470 nM
   TI
   LI
   LO
   TS
CP0035807
Cocaine
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C17H21NO4
 2
1
Ki = 524 nM
   TI
   LI
   LO
   TS
2
Ki = 965 nM
   TI
   LI
   LO
   TS
CP0452898
1-[3beta-(4-Thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]-1-[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylaminobenzene-4-yl]methane
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C45H48N4O2S2
 1
1
Ki = 730 nM
   TI
   LI
   LO
   TS
CP0528501
(2R,3S)-8-methyl-N-[4-[[(2S,3S)-8-methyl-3-(4-thiophen-3-ylphenyl)-8-azabicyclo[3.2.1]octane-2-carbonyl]amino]cyclohexyl]-3-(4-thiophen-3-ylphenyl)-8-azabicyclo[3.2.1]octane-2-carboxamide
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C44H52N4O2S2
 1
1
Ki = 810 nM
   TI
   LI
   LO
   TS
CP0452895
1,3-Di[3-(4-thiophene-3-yl-phenyl)tropane-2-carbonylaminomethyl]benzene
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C46H50N4O2S2
 1
1
Ki = 860 nM
   TI
   LI
   LO
   TS
CP0490974
1-[3beta-(4-Chlorophenyl)tropane-2beta-carbonyl-amino]-1-[3beta-(4-chlorophenyl)tropane-2beta-carbonyl-aminobenzene-4-yl]methane
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C37H42Cl2N4O2
 1
1
Ki = 1500 nM
   TI
   LI
   LO
   TS
CP0494736
1,6-Di[3beta-(4-thiophene-3-yl-phenyl)tropane-2beta-carbonylamino]hexane
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C44H54N4O2S2
 1
1
Ki = 2100 nM
   TI
   LI
   LO
   TS
CP0374073
1-[3beta-(4-Chlorophenyl)tropane-2beta-carbonyl-amino]-2-[3beta-(4-chlorophenyl)tropane-2beta-carbonyl-piperidine-4-yl]ethane
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C37H48Cl2N4O2
 1
1
Ki = 2500 nM
   TI
   LI
   LO
   TS
CP0374072
1-[3beta-(4-Chlorophenyl)tropane-2beta-carbonyl-amino]-2-[3beta-(4-chlorophenyl)tropane-2beta-carbonyl-aminobenzene-4-yl]ethane
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C38H44Cl2N4O2
 1
1
Ki = 2600 nM
   TI
   LI
   LO
   TS
CP0434093
methyl (3S,4R)-4-(4-iodophenyl)-1-methylpiperidine-3-carboxylate
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C14H18INO2
 1
1
Ki = 2810 nM
   TI
   LI
   LO
   TS
CP0405659
ethyl 4-(3-nitrophenyl)-1,2,3,6-tetrahydropyridine-5-carboxylate
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C14H16N2O4
 1
1
Ki = 3000 nM
   TI
   LI
   LO
   TS
CP0383047
1,4-Di[3beta-(4-chlorophenyl)tropane-2beta-carbonyl-amino]benzene
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C36H40Cl2N4O2
 1
1
Ki = 3200 nM
   TI
   LI
   LO
   TS
CP0491274
(2R,3S)-3-(4-chlorophenyl)-N-[4-[[(2S,3S)-3-(4-chlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carbonyl]amino]cyclohexyl]-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxamide
   Show/Hide
C36H46Cl2N4O2
 1
1
Ki = 4000 nM
   TI
   LI
   LO
   TS
CP0393073
furan-2-ylmethyl 2-(3,4-dichlorophenyl)cyclopentene-1-carboxylate
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C17H14Cl2O3
 1
1
Ki = 24000 nM
   TI
   LI
   LO
   TS
CP0453802
2-(3,4-dichlorophenyl)-N-(furan-2-ylmethyl)cyclopent-1-enecarboxamide
   Show/Hide
C17H15Cl2NO2
 1
1
Ki = 24000 nM
   TI
   LI
   LO
   TS
CP0462977
methyl (3S,4S)-1-methyl-4-phenylpiperidine-3-carboxylate
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C14H19NO2
 1
1
Ki = 27000 nM
   TI
   LI
   LO
   TS
CP0372547
methyl 2-(3-nitrophenyl)cyclohexene-1-carboxylate
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C14H15NO4
 1
1
Ki = 28700 nM
   TI
   LI
   LO
   TS
CP0439452
methyl 2-(4-phenylphenyl)cycloheptene-1-carboxylate
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C21H22O2
 1
1
Ki = 32000 nM
   TI
   LI
   LO
   TS
CP0485197
methyl (3S,4R)-1-methyl-4-phenylpiperidine-3-carboxylate
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C14H19NO2
 1
1
Ki = 46700 nM
   TI
   LI
   LO
   TS
CP0378279
2-hydroxyethyl 2-(3,4-dichlorophenyl)cyclopent-1-enecarboxylate
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C14H14Cl2O3
 1
1
Ki = 50000 nM
   TI
   LI
   LO
   TS
CP0467972
methyl (1R,2S)-2-(4-phenylphenyl)cycloheptane-1-carboxylate
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C21H24O2
 1
1
Ki = 73000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0077951
1-(2-(4-(6-fluoro-1H-indol-3-yl)-5,6-dihydropyridin-1(2H)-yl)ethyl)-3,4-dihydro-1H-isochromene-6-carboxamide
   Show/Hide
C25H26FN3O2
 1
1 IC50 = 0.11 nM
CP0354231
(+/-)-trans-3-(2-((dimethylamino)methyl)cyclopentyl)-1H-indole-5-carbonitrile
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C17H21N3
 1
1 IC50 = 0.13 nM
CP0035683
(1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine;hydrochloride
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C17H17Cl2N
 2
1 IC50 = 0.19 nM
2 Kd = 0.29 nM
CP0130783
(2-(3,4-dichlorophenoxy)phenyl)-N,N-dimethylmethanamine
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C15H15Cl2NO
 1
1 IC50 = 0.35 nM
CP0171392
(+)3-((1S,2S)-2-Dimethylaminomethyl-cyclopropyl)-1H-indole-5-carbonitrile
   Show/Hide
C15H17N3
 3
1 IC50 = 0.48 nM
2 Ki = 0.18 nM
3 Ki = 0.56 nM
CP0036757
3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
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C19H24N2
 16
1 IC50 = 1.1 nM
2 IC50 = 2 nM
3 IC50 = 3.5 nM
4 IC50 = 4.1 nM
5 IC50 = 4.4 nM
6 IC50 = 6.9 nM
7 IC50 = 7.3 nM
8 IC50 = 29 nM
9 Ki = 0.52 nM
10 Ki = 0.77 nM
11 Ki = 1.9 nM
12 Ki = 3.2 nM
13 Ki = 5 nM
14 Ki = 7.57 nM
15 Ki = 20 nM
16 Ki = 20.3 nM
CP0037455
(2-(4-chlorophenoxy)phenyl)-N,N-dimethylmethanamine
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C15H16ClNO
 1
1 IC50 = 1.68 nM
CP0050379
3-(3-(dimethylamino)propyl)-1H-indole-5-carbonitrile
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C14H17N3
 2
1 IC50 = 2 nM
2 Ki = 2 nM
CP0035258
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
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C17H18F3NO
 9
1 IC50 = 3.58 nM
2 IC50 = 180 nM
3 Kd = 0.81 nM
4 Ki = 0.72 nM
5 Ki = 2 nM
6 Ki = 2.2 nM
7 Ki = 3.17 nM
8 Ki = 3.5 nM
9 Ki = 48 nM
CP0048263
(1E)-5-methoxy-1-[4-(trifluoromethyl)phenyl]pentan-1-one O-(2-aminoethyl)oxime
   Show/Hide
C15H21F3N2O2
 1
1 IC50 = 3.8 nM
CP0054269
3-(5-fluoro-1H-indol-3-yl)-N,N-dimethylpropan-1-amine
   Show/Hide
C13H17FN2
 2
1 IC50 = 4 nM
2 Ki = 4 nM
CP0048839
(2S,3S)-methyl 3-(4-iodophenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate
   Show/Hide
C16H20INO2
 3
1 IC50 = 4.2 nM
2 IC50 = 4.21 nM
3 Ki = 0.38 nM
CP0008168
CAS_136434-34-9
   Show/Hide
C18H19NOS
 5
1 IC50 = 6.6 nM
2 Ki = 0.5012 nM
3 Ki = 0.79 nM
4 Ki = 0.8 nM
5 Ki = 4.6 nM
CP0121133
(S)-VENLAFAXINE
   Show/Hide
C17H27NO2
 2
1 IC50 = 7 nM
2 IC50 = 20 nM
CP0046644
rel-1-(3,4-dichlorophenyl)-6-(methoxymethyl)-3-azabicyclo[4.1.0]heptane
   Show/Hide
C14H17Cl2NO
 3
1 IC50 = 9.2 nM
2 Ki = 0.631 nM
3 Ki = 1.047 nM
CP0224231
AMITIFADINE HYDROCHLORIDE
   Show/Hide
C11H11Cl2N
 1
1 IC50 = 12.3 nM
CP0346800
(1S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
   Show/Hide
C11H11Cl2N
 1
1 IC50 = 13 nM
CP0041749
1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
   Show/Hide
C20H21FN2O
 3
1 IC50 = 13.41 nM
2 IC50 = 90 nM
3 Ki = 1.6 nM
CP0048099
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane
   Show/Hide
C11H11Cl2N
 3
1 IC50 = 13.8 nM
2 IC50 = 14 nM
3 Ki = 63 nM
CP0054778
CAS_93413-69-5
   Show/Hide
C17H27NO2
 2
1 IC50 = 20 nM
2 Kd = 8.9 nM
CP0046806
(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine
   Show/Hide
C19H20FNO3
 5
1 IC50 = 20 nM
2 Kd = 0.13 nM
3 Ki = 0.04 nM
4 Ki = 0.077 nM
5 Ki = 0.08 nM
CP0159508
1-[(1R)-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol
   Show/Hide
C17H27NO2
 1
1 IC50 = 30 nM
CP0067008
N-methyl-1-(1-naphthalen-2-ylcyclohexyl)methanamine
   Show/Hide
C18H23N
 1
1 IC50 = 34 nM
CP0341367
3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine
   Show/Hide
C13H18N2
 1
1 IC50 = 58 nM
CP0060502
1-(6-(methylthio)naphthalen-2-yl)propan-2-amine
   Show/Hide
C10H15NS
 1
1 IC50 = 74 nM
CP0037646
Midalcipran
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C15H22N2O
 2
1 IC50 = 100 nM
2 IC50 = 420 nM
CP0772168
N-(3-(4-Benzylpiperidin-1-yl)propyl)-2-naphthamide
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C26H30N2O
 1
1 IC50 = 100 nM
CP0116683
(2R,4R)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-2-amine
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C17H17Cl2N
 1
1 IC50 = 107 nM
CP0033479
(chloropromazine) [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine
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C17H19ClN2S
 1
1 IC50 = 120 nM
CP0189728
US9018211, 2A
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C26H30N2O6
 1
1 IC50 = 120 nM
CP0064806
(1S,5R)-1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane
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C11H11Cl2N
 1
1 IC50 = 133 nM
CP0038933
methyl (1R,2S,3S,5R)-3-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
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C16H20FNO2
 4
1 IC50 = 160 nM
2 IC50 = 692 nM
3 IC50 = 759 nM
4 Ki = 63 nM
CP0051444
1-(1-(3,4-dichlorophenyl)cyclohexyl)-N-methylmethanamine
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C14H19Cl2N
 1
1 IC50 = 169 nM
CP0051283
ATOMOXETINE
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C17H21NO
 2
1 IC50 = 190 nM
2 Kd = 8.9 nM
CP0035807
Cocaine
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C17H21NO4
 9
1 IC50 = 304 nM
2 IC50 = 1050 nM
3 Ki = 45 nM
4 Ki = 95 nM
5 Ki = 129 nM
6 Ki = 155 nM
7 Ki = 310 nM
8 Ki = 390 nM
9 Ki = 500 nM
CP0156540
(1S,2R)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide
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C15H22N2O
 1
1 IC50 = 320 nM
CP0010255
(RS)-3,4-(methylenedioxy)methamphetamine
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C11H15NO2
 1
1 IC50 = 425 nM
CP0228182
(+/-)2-Benzo[1,3]dioxol-5-yl-1-methyl-ethylamine
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C10H13NO2
 1
1 IC50 = 478 nM
CP0097042
Ansofaxine
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C24H31NO3
 1
1 IC50 = 723 nM
CP0159504
(2S)-2-(1-hydroxysilinan-1-yl)-2-(4-methoxyphenyl)-N,N-dimethylethanamine
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C16H27NO2Si
 1
1 IC50 = 791 nM
CP0046330
2-(1-hydroxysilinan-1-yl)-2-(4-methoxyphenyl)-N,N-dimethylethanamine
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C16H27NO2Si
 1
1 IC50 = 1063 nM
CP0068316
4-benzyl-1-[2-[bis(4-fluorophenyl)methoxy]ethyl]piperidine
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C27H29F2NO
 1
1 IC50 = 1670 nM
CP0109790
(R)-1-(2-(dimethylamino)-1-(4-methoxyphenyl)ethyl)silinan-1-ol
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C16H27NO2Si
 2
1 IC50 = 3168 nM
2 IC50 = 4200 nM
CP0103744
CAS_92623-85-3
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C15H22N2O
 1
1 IC50 = 3500 nM
CP0000055
2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one
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C13H18ClNO
 1
1 IC50 = 47000 nM
CP0068314
N-[3-(4-benzylpiperidin-1-yl)propyl]-2,2-diphenylacetamide
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C29H34N2O
 1
1 IC50 > 10000 nM
CP0136670
2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane
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C17H20INO2
 1
1 Ki = 0.04 nM
CP0039585
(1S,5S,6S)-1-(3,4-Dichlorophenyl)-6-[(ethyloxy)methyl]-3-azabicyclo-[3.1.0]hexane
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C14H17Cl2NO
 1
1 Ki = 0.1585 nM
CP0725880
(6R,11S)-11-(3,4-dichlorophenyl)-2-oxa-8-azaspiro[5.5]undecane
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C15H19Cl2NO
 1
1 Ki = 0.3162 nM
CP0183973
N-[2-[(6-fluoro-3,4-dihydro-2H-chromen-8-yl)oxy]ethyl]-3-(5-fluoro-1H-indol-3-yl)propan-1-amine
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C22H24F2N2O2
 2
1 Ki = 0.47 nM
2 Ki = 0.5 nM
CP0024732
5-{4-[4-(5-Cyano-1H-indol-3-yl)-butyl]-piperazin-1-yl}-benzofuran-2-carboxylic acid amide
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C26H27N5O2
 1
1 Ki = 0.5 nM
CP0302438
N-benzyl-N-piperidin-4-yl-1H-indol-5-amine
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C20H23N3
 1
1 Ki = 0.7943 nM
CP0041286
(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
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C20H21FN2O
 1
1 Ki = 1 nM
CP0229064
3-Amino-4-(2-dimethylaminomethyl-phenylsulfanyl)-benzonitrile
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C16H17N3S
 1
1 Ki = 1.1 nM
CP0689683
SID50106352
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C17H19ClF3NO
 1
1 Ki = 1.1 nM
CP0209926
3-{1-[2-(1H-Indol-4-yloxy)-ethyl]-1,2,3,6-tetrahydro-pyridin-4-yl}-1H-pyrrolo[2,3-b]pyridine
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C22H22N4O
 1
1 Ki = 1.5 nM
CP0658701
1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]-piperazine Hydrochloride
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C18H23ClN2S
 1
1 Ki = 1.6 nM
CP0104534
2-(2-((dimethylamino)methyl)phenylthio)-5-methylaniline
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C16H20N2S
 1
1 Ki = 1.65 nM
CP0354473
N-[2-[(6-fluoro-3,4-dihydro-2H-chromen-8-yl)oxy]ethyl]-2-(5-fluoro-1H-indol-3-yl)ethanamine
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C21H22F2N2O2
 1
1 Ki = 5 nM
CP0666771
(1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane hydrochloride
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C11H12Cl3N
 1
1 Ki = 15.85 nM
CP0055808
3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine
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C18H22N2
 1
1 Ki = 20 nM
CP0056386
5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one
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C21H21ClN4OS
 1
1 Ki = 53 nM
CP0119082
1-(2-benzhydryloxyethyl)-N-(3-phenylpropyl)piperidin-4-amine
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C29H36N2O
 1
1 Ki = 55 nM
CP0130302
1-(2-benzhydryloxyethyl)-N-methyl-N-(3-phenylpropyl)piperidin-4-amine
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C30H38N2O
 1
1 Ki = 87 nM
CP0042927
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
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C23H27Cl2N3O2
 3
1 Ki = 98 nM
2 Ki = 240 nM
3 Ki = 1080 nM
CP0063854
1-{2-[bis(4-fluorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine
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C28H32F2N2O
 2
1 Ki = 126 nM
2 Ki = 130 nM
CP0083053
2-(2-chloro-6-fluorophenoxy)-3-(piperidin-4-yl)pyridine
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C16H16ClFN2O
 1
1 Ki = 194 nM
CP0209068
(2-Benzhydryloxy-ethyl)-[1-(3-phenyl-propyl)-piperidin-3-ylmethyl]-amine
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C30H38N2O
 1
1 Ki = 210 nM
CP0150166
1-(2-benzhydryloxyethyl)-N-[2-(4-fluorophenyl)ethyl]piperidin-4-amine
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C28H33FN2O
 1
1 Ki = 220 nM
CP0196177
N-[[1-(2-benzhydryloxyethyl)piperidin-3-yl]methyl]-3-phenylpropan-1-amine
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C30H38N2O
 1
1 Ki = 320 nM
CP0076638
(2-Benzhydryloxy-ethyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-3-ylmethyl}-amine
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C29H35FN2O
 1
1 Ki = 350 nM
CP0002071
N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-N-prop-2-enylprop-2-en-1-amine
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C17H22N2O
 1
1 Ki = 501.19 nM
CP0209018
N-[[1-(2-benzhydryloxyethyl)piperidin-3-yl]methyl]-2-(4-fluorophenyl)-N-methylethanamine
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C30H37FN2O
 1
1 Ki = 530 nM
CP0049036
1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine
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C28H34N2O
 2
1 Ki = 620 nM
2 Ki = 2090 nM
CP0135012
(1R,2R)-N-[(2R,3R)-2-amino-3-methoxybutyl]-N-[4-[4-(methoxymethyl)phenyl]phenyl]-2-pyridin-2-ylcyclopropane-1-carboxamide;dihydrochloride
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C28H35Cl2N3O3
 1
1 Ki = 750 nM
CP0086307
(+)-2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine
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C16H18N2
 2
1 Ki = 874 nM
2 Ki = 2057 nM
CP0341416
N-[[1-(2-benzhydryloxyethyl)piperidin-3-yl]methyl]-2-(4-fluorophenyl)ethanamine
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C29H35FN2O
 1
1 Ki = 890 nM
CP0050766
(S)-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinolin-8-amine
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C16H18N2
 1
1 Ki = 935 nM
CP0055758
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine
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C17H17F2NO
 1
1 Ki = 1260 nM
CP0214425
(2-Benzhydryloxy-ethyl)-[1-(3-phenyl-propyl)-piperidin-4-yl]-amine
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C30H38N2O
 1
1 Ki = 1400 nM
CP0057295
(R)-Nomifensine
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C16H18N2
 1
1 Ki = 1550 nM
CP0041678
(2-Benzhydryloxy-ethyl)-(1-benzyl-piperidin-4-yl)-amine
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C27H32N2O
 1
1 Ki = 2160 nM
CP0042099
5-[(3,4-dimethoxyphenyl)methyl]-5-azahexacyclo[5.4.1.02,6.03,10.04,8.09,12]dodecan-4-ol
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C20H23NO3
 1
1 Ki = 4421 nM
Clinical Information about the Protein
Target 1 ( Serotonin transporter (SERT) )
Target Type Successful Target
Disease 13 Target-related Diseases  13
1 Pain [ICD-11: MG30-MG3Z]
2 Depression [ICD-11: 6A70-6A7Z]
3 Smoking dependence [ICD-11: 6C4A.2]
4 Anaesthesia [ICD-11: 9A78.6]
5 Major depressive disorder [ICD-11: 6A70.3]
6 Fibromyalgia [ICD-11: MG30.01]
7 Anxiety disorder [ICD-11: 6B00-6B0Z]
8 Obesity [ICD-11: 5B81]
9 Neuropathic pain [ICD-11: 8E43.0]
10 Insomnia [ICD-11: 7A00-7A0Z]
11 Mood disorder [ICD-11: 6A60-6E23]
12 Inflammation [ICD-11: 1A00-CA43.1]
13 Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
Approved Drug(s) 22 Approved Drugs  22
1 Acetaminophen Approved
Pain
2 Amitriptyline Approved
Depression
3 Bupropion Approved
Smoking dependence
4 Citalopram Approved
Depression
5 Clomipramine Approved
Depression
6 Cocaine Approved
Anaesthesia
7 Desvenlafaxine Approved
Major depressive disorder
8 Duloxetine Approved
Depression
9 Escitalopram Approved
Major depressive disorder
10 Fluoxetine Approved
Depression
11 Fluvoxamine Approved
Depression
12 Levomilnacipran Approved
Fibromyalgia
13 Luvox Approved
Anxiety disorder
14 Nortriptyline Approved
Depression
15 Paroxetine Approved
Depression
16 Sertraline Approved
Depression
17 Sibutramine Approved
Obesity
18 Tianeptine Approved
Major depressive disorder
19 Trazodone Approved
Depression
20 Venlafaxine Approved
Depression
21 Vilazodone Approved
Major depressive disorder
22 Vortioxetine Approved
Major depressive disorder
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 Amitifadine Phase 3
Obesity
2 Bicifadine Phase 3
Neuropathic pain
3 ITI-007 Phase 3
Insomnia
4 LITOXETINE Phase 3
Mood disorder
Discontinued Drug(s) 5 Discontinued Drugs  5
1 Dexfenfluramine Withdrawn from market
Obesity
2 ZIMELIDINE Withdrawn from market
Major depressive disorder
3 DOV-216303 Discontinued in Phase 2
Mood disorder
4 YM-992 Discontinued in Phase 2
Depression
5 Irindalone Terminated
Inflammation
Investigative Drug(s) 2 Investigative Drugs  2
1 PF-3409409 Investigative
Attention deficit hyperactivity disorder
2 S33005 Investigative
Depression
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00891 Sodium-dependent serotonin transporter Rattus norvegicus, Rat
PT01609 Sodium-dependent serotonin transporter Mus musculus, Mouse