General Information of the Protein
Protein ID
PT01354
Protein Name
5-hydroxytryptamine receptor 6
Secondarily
Protein Name
Serotonin receptor 6
Gene Name
HTR6
Sequence
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNTSNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLISLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQCRLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVPRTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPGLFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGPRPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNFFNIDPAEPELRPHPLGIPTN
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Serotonin receptor
Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of TOR signaling (PubMed:23027611).
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Uniprot ID
Primary ID:
P50406

Secondarily ID:
Q13640
Q5TGZ1
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Ensembl ID
ENSG00000158748
HGNC ID
HGNC:5301
Subcellular Location
Cell 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: CL000094 , 1321N1
Compound ID Compound Name Compound Formula
CP0041613
Anapriline
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C16H21NO2
 2
1
EC50 > 5011.87 nM
   TI
   LI
   LO
   TS
2
IC50 > 5011.87 nM
   TI
   LI
   LO
   TS
CP0066236
1-(dimethylamino)-3-[(2-methyl-1H-1,2-benzazaborinin-8-yl)oxy]propan-2-ol
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C14H21BN2O2
 2
1
EC50 > 5011.87 nM
   TI
   LI
   LO
   TS
2
IC50 > 5011.87 nM
   TI
   LI
   LO
   TS
CP0366351
1-(dimethylamino)-3-[(2-methyl-1H-1,2-benzazaborinin-5-yl)oxy]propan-2-ol
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C14H21BN2O2
 2
1
EC50 > 5011.87 nM
   TI
   LI
   LO
   TS
2
IC50 > 5011.87 nM
   TI
   LI
   LO
   TS
CP0073333
3-benzenesulfonyl-8-piperazin-1-ylquinoline
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C19H19N3O2S
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0565805
1-(3-chlorophenyl)sulfonyl-4-piperazin-1-yl-2-propan-2-ylimidazo[4,5-c]pyridine
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C19H22ClN5O2S
 1
1
IC50 = 5.2 nM
   TI
   LI
   LO
   TS
CP0515605
1-(3-chlorophenyl)sulfonyl-2-ethyl-4-piperazin-1-ylimidazo[4,5-c]pyridine
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C18H20ClN5O2S
 1
1
IC50 = 5.4 nM
   TI
   LI
   LO
   TS
CP0537527
2-ethyl-1-(3-fluorophenyl)sulfonyl-4-piperazin-1-ylimidazo[4,5-c]pyridine
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C18H20FN5O2S
 1
1
IC50 = 6.4 nM
   TI
   LI
   LO
   TS
CP0548230
1-(3-chlorophenyl)sulfonyl-4-piperazin-1-ylimidazo[4,5-c]pyridine
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C16H16ClN5O2S
 1
1
IC50 = 6.6 nM
   TI
   LI
   LO
   TS
CP0552195
1-(3-chlorophenyl)sulfonyl-2-phenyl-4-piperazin-1-ylimidazo[4,5-c]pyridine
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C22H20ClN5O2S
 1
1
IC50 = 10.6 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0153460
2-(5-chloro-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine
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C13H17ClN2
 1
1 EC50 = 44.8 nM
CP0175237
5-(benzenesulfonyl)-N,11-dimethyl-2,3,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7-tetraen-4-amine
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C17H19N5O2S
 2
1 IC50 = 0.837 nM
2 Ki = 0.389 nM
CP0226262
4-(benzenesulfonyl)-N,8,11-trimethyl-2,6,7,11-tetrazatricyclo[7.4.0.03,7]trideca-1,3,5,8-tetraen-5-amine
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C18H21N5O2S
 2
1 IC50 = 1.43 nM
2 Ki = 0.662 nM
CP0329025
5-(benzenesulfonyl)-N,8,11-trimethyl-2,3,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7-tetraen-4-amine
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C18H21N5O2S
 2
1 IC50 = 1.48 nM
2 Ki = 0.685 nM
CP0037955
METHIOTHEPIN
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C20H24N2S2
 2
1 IC50 = 2.4 nM
2 Ki = 0.4 nM
CP0304087
2-(benzenesulfonyl)-N-ethyl-5-piperazin-1-ylaniline
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C18H23N3O2S
 1
1 IC50 = 2.7 nM
CP0043132
3-Benzenesulfonyl-2-methylsulfanyl-pyrido[1,2-a]pyrimidin-(4E)-ylideneamine
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C15H13N3O2S2
 2
1 IC50 = 4 nM
2 Ki = 3.981 nM
CP0219258
5,7-dimethyl-2-(methylthio)-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine
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C15H15N3O2S2
 5
1 IC50 = 4.61 nM
2 IC50 = 30 nM
3 Ki = 2 nM
4 Ki = 2.1 nM
5 Ki = 2.14 nM
CP0016259
4-(benzenesulfonyl)-N,11-dimethyl-2,6,7,11-tetrazatricyclo[7.4.0.03,7]trideca-1,3,5,8-tetraen-5-amine
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C17H19N5O2S
 2
1 IC50 = 7.02 nM
2 Ki = 3.26 nM
CP0077916
5-Chloro-2-methyl-3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indole
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C14H15ClN2
 1
1 IC50 = 7.4 nM
CP0326089
3-(4-fluorophenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C15H14FN3O2S2
 2
1 IC50 < 10 nM
2 IC50 = 112 nM
CP0513900
5-(benzenesulfonyl)-4,11-dimethyl-2,3,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7-tetraene
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C17H18N4O2S
 2
1 IC50 = 13 nM
2 Ki = 60 nM
CP0073332
2-ethyl-3-[(3-fluorophenyl)methyl]-7-piperazin-1-ylimidazo[4,5-b]pyridine
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C19H22FN5
 2
1 IC50 = 17.6 nM
2 Ki = 6 nM
CP0126985
3-(3-chlorophenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C15H14ClN3O2S2
 1
1 IC50 = 20 nM
CP0126984
3-(3-fluorophenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C15H14FN3O2S2
 1
1 IC50 = 25 nM
CP0118951
4-Amino-N-(2,6-bis-dimethylamino-pyrimidin-4-yl)-benzenesulfonamide
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C12H16N6O2S
 5
1 IC50 = 26.3 nM
2 Ki = 50.12 nM
3 Ki = 54.95 nM
4 Ki = 55 nM
5 Ki = 58 nM
CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
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C10H12N2O
 11
1 IC50 = 27.5 nM
2 IC50 = 100 nM
3 IC50 = 180 nM
4 IC50 = 200 nM
5 IC50 = 262 nM
6 Ki = 50 nM
7 Ki = 65 nM
8 Ki = 70 nM
9 Ki = 84 nM
10 Ki = 93 nM
11 Ki = 100 nM
CP0126986
3-(3-chloro-4-fluorophenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C15H13ClFN3O2S2
 1
1 IC50 = 46 nM
CP0175239
5,7-Dimethyl-2-(ethylthio)-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidine
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C16H17N3O2S2
 1
1 IC50 = 50 nM
CP0306929
3-Benzenesulfonyl-2-methylsulfanyl-pyrimido[2,1-a]isoquinolin-(4Z)-ylideneamine
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C19H15N3O2S2
 1
1 IC50 = 68.9 nM
CP0154123
3-Benzenesulfonyl-8-ethyl-2-methylsulfanyl-pyrido[1,2-a]pyrimidin-(4Z)-ylideneamine
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C17H17N3O2S2
 1
1 IC50 = 70.1 nM
CP0293425
5-(benzenesulfonyl)-11-methyl-4-methylsulfanyl-2,3,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7-tetraene
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C17H18N4O2S2
 2
1 IC50 = 76.9 nM
2 Ki = 35.7 nM
CP0063547
2-Methylsulfanyl-3-(naphthalene-2-sulfonyl)-pyrido[1,2-a]pyrimidin-(4Z)-ylideneamine
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C19H15N3O2S2
 1
1 IC50 = 79.2 nM
CP0099428
5-Methoxy-2-methyl-3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indole
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C15H18N2O
 1
1 IC50 = 80 nM
CP0080534
2-ethyl-5-methoxy-N,N-dimethyltryptamine
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C15H22N2O
 3
1 IC50 = 85 nM
2 Ki = 16 nM
3 Ki < 50 nM
CP0281465
3-Benzenesulfonyl-7-fluoro-2-methylsulfanyl-pyrido[1,2-a]pyrimidin-(4Z)-ylideneamine
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C15H12FN3O2S2
 1
1 IC50 = 87.6 nM
CP0172993
2,5,7-Triimethyl-phenylsulfonyl-pyrazolo[1,5-a]pyrimidine
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C15H15N3O2S
 2
1 IC50 = 147 nM
2 Ki = 68.4 nM
CP0172992
3-(4-chlorophenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C15H14ClN3O2S2
 1
1 IC50 = 230 nM
CP0363770
3-Benzenesulfonyl-9-bromo-7-methyl-2-methylsulfanyl-pyrido[1,2-a]pyrimidin-(4Z)-ylideneamine
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C16H14BrN3O2S2
 1
1 IC50 = 269 nM
CP0293306
3-(4-methoxyphenyl)sulfonyl-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine
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C16H17N3O3S2
 1
1 IC50 = 440 nM
CP0223269
2-{[5,7-Dimethyl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidin-2-yl]oxy}ethanol
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C16H17N3O4S
 3
1 IC50 = 477 nM
2 Ki = 22.2 nM
3 Ki = 222 nM
CP0211753
5,7-Dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidine
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C14H13N3O2S
 3
1 IC50 = 510 nM
2 IC50 > 1000 nM
3 Ki = 237 nM
CP0321822
4-(benzenesulfonyl)-11-methyl-5-methylsulfanyl-2,6,7,11-tetrazatricyclo[7.4.0.03,7]trideca-1,3,5,8-tetraene
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C17H18N4O2S2
 2
1 IC50 = 801 nM
2 Ki = 372 nM
CP0513899
4-(4-fluorophenyl)sulfonyl-11-methyl-5-methylsulfanyl-2,6,7,11-tetrazatricyclo[7.4.0.03,7]trideca-1,3,5,8-tetraene
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C17H17FN4O2S2
 1
1 IC50 > 1000 nM
CP0216239
3-(benzenesulfonyl)-N,5,7-trimethylpyrazolo[1,5-a]pyrimidin-2-amine
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C15H16N4O2S
 1
1 Ki = 0.2 nM
CP0073333
3-benzenesulfonyl-8-piperazin-1-ylquinoline
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C19H19N3O2S
 4
1 Ki = 0.23 nM
2 Ki = 0.234 nM
3 Ki = 0.25 nM
4 Ki = 0.28 nM
CP0523047
1-(benzenesulfonyl)-2-methyl-4-piperazin-1-ylbenzimidazole
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C18H20N4O2S
 2
1 Ki = 0.5 nM
2 Ki = 0.53 nM
CP0214694
2-(2,6-difluorophenyl)-6-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]pyridazin-3-one
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C25H23F3N4O3
 1
1 Ki = 0.5 nM
CP0339112
4-phenyl-N-(4-piperazin-1-ylquinolin-6-yl)benzenesulfonamide
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C25H24N4O2S
 1
1 Ki = 0.5012 nM
CP0043595
(3R)-N,N-Dimethyl-1-[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
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C23H24N4O2S
 1
1 Ki = 0.51 nM
CP0265775
6-chloro-N-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]imidazo[2,1-b][1,3]thiazole-5-sulfonamide
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C17H18ClN5O2S2
 3
1 Ki = 0.58 nM
2 Ki = 2.2 nM
3 Ki = 312 nM
CP0113176
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide
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C21H24ClN3O3S2
 2
1 Ki = 0.6 nM
2 Ki = 0.631 nM
CP0081712
4-tert-butyl-N-(4-piperazin-1-ylquinolin-6-yl)benzenesulfonamide
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C23H28N4O2S
 1
1 Ki = 0.631 nM
CP0041243
5-chloro-N-[4-methoxy-3-(piperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride
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C20H22ClN3O3S2
 3
1 Ki = 0.66 nM
2 Ki = 1 nM
3 Ki = 1.259 nM
CP0294753
9-methyl-2-(methylthio)-3-(phenylsulfonyl)-5,6,7,8-tetrahydropyrazolo[5,1-b]quinazoline
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C18H19N3O2S2
 1
1 Ki = 0.68 nM
CP0037941
2-[1-(Naphthalene-1-sulfonyl)-1H-indol-6-yl]-octahydro-pyrrolo[1,2-a]pyrazine
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C25H25N3O2S
 1
1 Ki = 0.7 nM
CP0309013
5-chloro-N-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]naphthalene-2-sulfonamide
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C22H22ClN3O2S
 1
1 Ki = 0.7 nM
CP0199114
SB-399885
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C18H21Cl2N3O4S
 2
1 Ki = 0.7762 nM
2 Ki = 0.8 nM
CP0165719
N-[3-[(8aR)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-methoxyphenyl]-5-chloro-3-methyl-1-benzothiophene-2-sulfonamide
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C23H26ClN3O3S2
 1
1 Ki = 0.7943 nM
CP0183577
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid ((S)-3-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl-4-methoxy-phenyl)-amide
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C23H26ClN3O3S2
 2
1 Ki = 0.7943 nM
2 Ki = 0.8 nM
CP0258948
4-(3-(2-(dimethylamino)ethyl)-1H-indol-1-ylsulfonyl)benzenamine
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C18H21N3O2S
 1
1 Ki = 0.8 nM
CP0217150
IDALOPIRDINE
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C20H19F5N2O
 1
1 Ki = 0.83 nM
CP0093674
3-(3-bromo-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18BrN3O2S
 1
1 Ki = 0.8913 nM
CP0279831
2-(5-methoxy-1-naphthalen-1-ylsulfonylindol-3-yl)-N,N-dimethylethanamine
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C23H24N2O3S
 1
1 Ki = 0.9 nM
CP0111551
5-chloro-N-(4-piperazin-1-ylquinolin-6-yl)naphthalene-2-sulfonamide
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C23H21ClN4O2S
 1
1 Ki = 1 nM
CP0208303
5-chloro-2-methyl-N-(4-piperazin-1-ylquinolin-6-yl)-1-benzothiophene-3-sulfonamide
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C22H21ClN4O2S2
 1
1 Ki = 1 nM
CP0306083
5-chloro-3-methyl-N-[4-(4-methylpiperazin-1-yl)quinolin-6-yl]-1-benzothiophene-2-sulfonamide
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C23H23ClN4O2S2
 1
1 Ki = 1 nM
CP0039674
1-(2-bromophenyl)sulfonyl-3-(1-methylpyrrolidin-3-yl)indole
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C19H19BrN2O2S
 1
1 Ki = 1 nM
CP0777252
2-Iodo-N-(3-(R)-1-pyrrolidin-2-ylmethyl-1H-indol-5-yl)-benzenesulfonamide
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C20H22IN3O2S
 1
1 Ki = 1 nM
CP0144979
1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole
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C18H19N3O2S
 1
1 Ki = 1 nM
CP0237538
2,8-Dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
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C21H24N2
 1
1 Ki = 1.2 nM
CP0113794
3-[(5-chlorothien-2-yl)sulfonyl]-1-piperidin-3-yl-1H-pyrrolo[2,3-b]pyridine
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C16H16ClN3O2S2
 1
1 Ki = 1.202 nM
CP0082421
5-chloro-3-methyl-N-(2-methyl-4-piperazin-1-ylquinolin-6-yl)-1-benzothiophene-2-sulfonamide
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C23H23ClN4O2S2
 1
1 Ki = 1.259 nM
CP0170807
5-chloro-3-ethyl-N-(4-piperazin-1-ylquinolin-6-yl)-1-benzothiophene-2-sulfonamide
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C23H23ClN4O2S2
 1
1 Ki = 1.259 nM
CP0343547
5-chloro-3-methyl-N-[4-[(3S)-3-methylpiperazin-1-yl]quinolin-6-yl]-1-benzothiophene-2-sulfonamide
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C23H23ClN4O2S2
 1
1 Ki = 1.259 nM
CP0281706
6-(1,2,3,5,8,8a-Hexahydro-indolizin-7-yl)-1-(naphthalene-1-sulfonyl)-1H-indole
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C26H24N2O2S
 1
1 Ki = 1.259 nM
CP0302411
3-(3-bromo-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16BrN3O2S
 1
1 Ki = 1.288 nM
CP0309906
3-[(3-chlorophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 1.288 nM
CP0325789
1-pyrrolidin-3-yl-3-(3-trifluoromethyl-benzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine
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C18H16F3N3O2S
 1
1 Ki = 1.288 nM
CP0286684
(2-{2-[3-(3-Methoxy-benzyl)-[1,2,4]oxadiazol-5-yl]-1H-indol-3-yl}-ethyl)-dimethyl-amine
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C22H24N4O2
 1
1 Ki = 1.3 nM
CP0080114
Cerlapirdine
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C22H23N3O3S
 1
1 Ki = 1.3 nM
CP0318500
5-(1,4-diazepan-1-yl)-2-(4-fluorophenylsulfonyl)-N-methylbenzenamine
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C18H22FN3O2S
 1
1 Ki = 1.4 nM
CP0045070
1-Benzenesulfonyl-5-chloro-3-((R)-1-methyl-pyrrolidin-2-ylmethyl)-1H-indole
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C20H21ClN2O2S
 2
1 Ki = 1.4 nM
2 Ki < 50 nM
CP0302413
3-(3-fluoro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18FN3O2S
 1
1 Ki = 1.413 nM
CP0148437
(9-Benzenesulfonyl-6-methoxy-2,3,4,9-tetrahydro-1H-carbazol-4-ylmethyl)-dimethyl-amine
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C22H26N2O3S
 2
1 Ki = 1.5 nM
2 Ki = 2.3 nM
CP0330654
2-[1-(benzenesulfonyl)indol-4-yl]-N,N-dimethylethanamine
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C18H20N2O2S
 1
1 Ki = 1.5 nM
CP0275252
3-(3-chloro-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16ClN3O2S
 1
1 Ki = 1.514 nM
CP0288554
3-(3-chloro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 1.514 nM
CP0152148
2-(5-methoxy-1-naphthalen-2-ylsulfonylindol-3-yl)-N,N-dimethylethanamine
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C23H24N2O3S
 1
1 Ki = 1.6 nM
CP0076188
1-(benzenesulfonyl)-4,5-dihydro-3H-benzo[cd]indol-4-amine
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C17H16N2O2S
 1
1 Ki = 1.6 nM
CP0287755
3-[(5-chlorothien-2-yl)sulfonyl]-1-(1-methylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C17H18ClN3O2S2
 1
1 Ki = 1.905 nM
CP0173778
5-chloro-3-methyl-N-(4-piperazin-1-ylquinolin-6-yl)-1-benzothiophene-2-sulfonamide
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C22H21ClN4O2S2
 1
1 Ki = 1.995 nM
CP0310111
6-Chloro-imidazo[2,1-b]thiazole-5-sulfonic acid [1-(2-dimethylamino-ethyl)-1H-indol-5-yl]-amide
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C17H18ClN5O2S2
 1
1 Ki = 1.995 nM
CP0277694
3-[(2-fluorophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18FN3O2S
 1
1 Ki = 1.995 nM
CP0325786
3-(2-fluoro-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16FN3O2S
 1
1 Ki = 1.995 nM
CP0045069
2-[1-(benzenesulfonyl)-5-methoxyindol-3-yl]-N,N-dimethylethanamine
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C19H22N2O3S
 5
1 Ki = 2 nM
2 Ki = 2.1 nM
3 Ki = 2.3 nM
4 Ki = 2.512 nM
5 Ki < 50 nM
CP0144949
2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulfonyl)-1H-indol-3-yl]ethan-1-amine
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C15H13ClN4O2S2
 2
1 Ki = 2 nM
2 Ki = 2.2 nM
CP0093677
3-{[3-(trifluoromethyl)phenyl]sulfonyl}-1-(1-methylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C20H20F3N3O2S
 1
1 Ki = 2.089 nM
CP0648533
N-(3-Fluorophenyl)-2-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-sulfonamide hydrochloride
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C18H19ClFN3O2S
 1
1 Ki = 2.1 nM
CP0357075
3-(2-Chloro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 2.188 nM
CP0271608
3-[(3-fluorophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18FN3O2S
 1
1 Ki = 2.399 nM
CP0310110
SB-258585
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C18H22IN3O3S
 1
1 Ki = 2.512 nM
CP0325791
3-benzenesulfonyl-1-(1-methyl-pyrrolidin-3-yl)-1Hpyrrolo[2,3-b]pyridine
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C18H19N3O2S
 1
1 Ki = 2.512 nM
CP0276427
10-(benzenesulfonyl)-11-methylsulfanyl-2-piperazin-1-yl-1,8,12-triazatricyclo[7.3.0.03,7]dodeca-2,7,9,11-tetraene
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C20H23N5O2S2
 1
1 Ki = 2.512 nM
CP0316409
3-(3-fluoro-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16FN3O2S
 1
1 Ki = 2.692 nM
CP0285245
2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine
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C20H23N
 1
1 Ki = 3 nM
CP0099906
N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide
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C17H18Br2FN3O3S
 2
1 Ki = 3 nM
2 Ki = 3.162 nM
CP0277626
(3S)-1-[3-(1-Naphthylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
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C21H20N4O2S
 1
1 Ki = 3.06 nM
CP0255950
2-[1-(benzenesulfonyl)indol-3-yl]-N,N-dimethylethanamine
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C18H20N2O2S
 2
1 Ki = 3.162 nM
2 Ki = 4.1 nM
CP0326103
1-(1-ethylpiperidin-3-yl)-3-[(5-chlorothien-2-yl)-sulfonyl]-1H-pyrrolo[2,3-b]pyridine
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C18H20ClN3O2S2
 1
1 Ki = 3.236 nM
CP0093676
3-(3-chloro-benzenesulfonyl)-1-(1-ethyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C19H20ClN3O2S
 1
1 Ki = 3.311 nM
CP0143099
3-[(3-fluorophenyl)sulfonyl]-1-(1-isopropylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C21H24FN3O2S
 1
1 Ki = 3.388 nM
CP0277627
1-[3-(1-Naphthylsulfonyl)-1H-indazol-5-yl]azetidin-3-amine
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C20H18N4O2S
 1
1 Ki = 3.55 nM
CP0148007
1-{3-[(4-Methyl-1-naphthyl)sulfonyl]-1H-indazol-5-yl}piperidin-4-amine
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C23H24N4O2S
 1
1 Ki = 3.62 nM
CP0427370
1-(1-ethylpiperidin-3-yl)-3-(phenylsulfonyl)-1Hpyrrolo[2,3-b]pyridine
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C20H23N3O2S
 1
1 Ki = 3.631 nM
CP0291339
3-[(2-chlorophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 3.715 nM
CP0295962
3-[(3-bromophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18BrN3O2S
 1
1 Ki = 3.802 nM
CP0287714
3-[(3,5-dichlorophenyl)sulfonyl]-1-(1-methylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C19H19Cl2N3O2S
 1
1 Ki = 3.89 nM
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
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C18H19ClN4
 6
1 Ki = 4 nM
2 Ki = 9.5 nM
3 Ki = 10 nM
4 Ki = 11 nM
5 Ki < 50 nM
6 Ki = 100 nM
CP0033479
(chloropromazine) [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine
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C17H19ClN2S
 2
1 Ki = 4 nM
2 Ki < 50 nM
CP0379692
3-(4-methylpiperazin-1-yl)-1-(phenylsulfonyl)-1H-indole
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C19H21N3O2S
 1
1 Ki = 4 nM
CP0424546
N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methylsulfonyl-5-piperazin-1-ylaniline
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C21H28ClN3O4S
 1
1 Ki = 4 nM
CP0089877
3-(4-chloro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 4.169 nM
CP0093693
3-(4-bromo-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16BrN3O2S
 1
1 Ki = 4.266 nM
CP0309914
1-[3-(1-Naphthylsulfonyl)-1H-indazol-5-yl]piperidin-4-amine
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C22H22N4O2S
 1
1 Ki = 4.27 nM
CP0061587
1-(1-ethylpiperidin-3-yl)-3-[(3-fluorophenyl)sulfonyl]-1H-pyrrolo[2,3-b]pyridine
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C20H22FN3O2S
 1
1 Ki = 4.365 nM
CP0038773
(3R)-1-[3-(1-Naphthylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
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C21H20N4O2S
 1
1 Ki = 4.46 nM
CP0039675
6-chloro-N-[3-[2-(dimethylamino)ethyl]-2-methyl-1H-inden-5-yl]imidazo[2,1-b][1,3]thiazole-5-sulfonamide
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C19H21ClN4O2S2
 1
1 Ki = 4.5 nM
CP0062984
1-{3-[(5-Chloro-1-naphthyl)sulfonyl]-1H-indazol-5-yl}piperidin-4-amine
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C22H21ClN4O2S
 1
1 Ki = 4.52 nM
CP0295961
3-{[3-(trifluoromethyl)phenyl]sulfonyl}-1-piperidin-3-yl-1H-pyrrolo[2,3-b]pyridine
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C19H18F3N3O2S
 1
1 Ki = 4.571 nM
CP0158829
3-[(3-fluorophenyl)sulfonyl]-1-(1-methylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C19H20FN3O2S
 1
1 Ki = 4.677 nM
CP0271606
3-(phenylsulfonyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H19N3O2S
 1
1 Ki = 4.898 nM
CP0285020
2-(7-methoxy-1-naphthalen-2-ylsulfonylindol-3-yl)-N,N-dimethylethanamine
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C23H24N2O3S
 1
1 Ki = 5 nM
CP0185590
4-Bromo-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzenesulfonamide
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C18H22BrN3O3S
 1
1 Ki = 5 nM
CP0287843
3-(4-fluoro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18FN3O2S
 1
1 Ki = 5.012 nM
CP0325788
3-(4-chloro-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16ClN3O2S
 1
1 Ki = 5.495 nM
CP0218398
6-[5-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]pentanoyl]-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-11-one
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C28H30FN3O3
 1
1 Ki = 5.55 nM
CP0317149
6-[4-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]butanoyl]-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-11-one
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C27H28FN3O3
 1
1 Ki = 5.6 nM
CP0277693
3-(2-fluoro-benzenesulfonyl)-1-(1-methyl-pyrrolidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C18H18FN3O2S
 1
1 Ki = 5.623 nM
CP0647677
2,5-Dimethyl-8-(phenylsulfonyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole hydrochloride
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C19H21ClN2O2S
 1
1 Ki = 5.7 nM
CP0269589
8-(1-pyrrolidin-3-yl-1H-pyrrolo[2,3-b]pyridine-3-sulfonyl)-quinoline
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C20H18N4O2S
 1
1 Ki = 5.754 nM
CP0149650
2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine
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C19H22N2
 1
1 Ki = 6 nM
CP0294388
3-[(3,5-dichlorophenyl)sulfonyl]-1-piperidin-3-yl-1H-pyrrolo[2,3-b]pyridine
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C18H17Cl2N3O2S
 1
1 Ki = 6.166 nM
CP0045725
(4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide
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C20H25N3O
 1
1 Ki = 6.9 nM
CP0186950
(4S,5S)-4-Dimethylamino-1-(toluene-4-sulfonyl)-1,3,4,5-tetrahydro-benzo[cd]indol-5-ol
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C20H22N2O3S
 2
1 Ki = 7.2 nM
2 Ki = 7.943 nM
CP0271607
3-[(4-chlorophenyl)sulfonyl]-1-piperidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C18H18ClN3O2S
 1
1 Ki = 7.586 nM
CP0087260
3-[1-(benzenesulfonyl)indol-4-yl]-N,N-dimethylpropan-1-amine
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C19H22N2O2S
 1
1 Ki = 7.9 nM
CP0282297
1-(3-(3-chlorophenylsulfonyl)-1H-indazol-5-yl)piperidin-4-amine
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C18H19ClN4O2S
 1
1 Ki = 8.04 nM
CP0113787
1-(1-ethyl-pyrrolidin-3-yl)-3-(3-fluoro-benzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine
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C19H20FN3O2S
 1
1 Ki = 8.318 nM
CP0143094
3-(4-fluoro-benzenesulfonyl)-1-pyrrolidin-3-yl-1Hpyrrolo[2,3-b]pyridine
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C17H16FN3O2S
 1
1 Ki = 8.511 nM
CP0104220
3-[(3-bromophenyl)sulfonyl]-1-(1-isopropylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C21H24BrN3O2S
 1
1 Ki = 9.333 nM
CP0039676
4-indol-1-ylsulfonylaniline
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C14H12N2O2S
 1
1 Ki = 10 nM
CP0174706
6-chloro-N-[3-[2-(dimethylamino)ethyl]-1H-inden-5-yl]imidazo[2,1-b][1,3]thiazole-5-sulfonamide
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C18H19ClN4O2S2
 1
1 Ki = 10 nM
CP0045063
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine
   Show/Hide
C17H20N4S
 3
1 Ki = 10 nM
2 Ki = 10.7 nM
3 Ki < 50 nM
CP0291338
3-benzenesulfonyl-1-(1-ethyl-pyrrolidin-3-yl)-1Hpyrrolo[2,3-b]pyridine
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C19H21N3O2S
 1
1 Ki = 10.96 nM
CP0143098
3-[(4-chlorophenyl)sulfonyl]-1-(1-isopropylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C21H24ClN3O2S
 1
1 Ki = 11.22 nM
CP0093694
3-[(4-chlorophenyl)sulfonyl]-1-(1-methylpiperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine
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C19H20ClN3O2S
 1
1 Ki = 11.48 nM
CP0080436
4-Amino-N-(2,6-bis-methylamino-pyridin-4-yl)-benzenesulfonamide
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C13H17N5O2S
 2
1 Ki = 12 nM
2 Ki = 15.85 nM
CP0297596
3-{[4-(trifluoromethyl)phenyl]sulfonyl}-1-piperidin-3-yl-1H-pyrrolo[2,3-b]pyridine
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C19H18F3N3O2S
 1
1 Ki = 12.02 nM
CP0214619
1-{3-[(4-Isopropylphenyl)sulfonyl]-1H-indazol-5-yl}piperidin-4-amine
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C21H26N4O2S
 1
1 Ki = 13.09 nM
CP0295963
1-(1-ethylpiperidin-3-yl)-3-[(3,5-dichlorophenyl)-sulfonyl]-1H-pyrrolo[2,3-b]pyridine
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C20H21Cl2N3O2S
 1
1 Ki = 13.49 nM
CP0229727
(3R)-1-[1-(1-Methylethyl)-3-(naphthalen-1-ylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
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C24H26N4O2S
 1
1 Ki = 13.7 nM
CP0071154
2-(5-methoxy-1H-indol-3-yl)-N,N-dimethyl-ethanamine
   Show/Hide
C13H18N2O
 2
1 Ki = 16 nM
2 Ki = 70 nM
CP0102529
[3-[2-(dimethylamino)ethyl]-5-methoxyindol-1-yl]-phenylmethanone
   Show/Hide
C20H22N2O2
 2
1 Ki = 18 nM
2 Ki = 25.12 nM
CP0073585
1-[3-(2-Naphthylsulfonyl)-1H-indazol-5-yl]piperidin-4-amine
   Show/Hide
C22H22N4O2S
 1
1 Ki = 18.22 nM
CP0135451
2-(5-methoxy-2-phenyl-1H-indol-3-yl)-N,N-dimethylethanamine
   Show/Hide
C19H22N2O
 2
1 Ki = 20 nM
2 Ki = 50.12 nM
CP0318039
3-(2-Dimethylamino-ethyl)-1H-indole-2-carboxylic acid ethyl ester
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C15H20N2O2
 1
1 Ki = 20 nM
CP0148894
(3R)-1-[1-Methyl-3-(naphthalen-1-ylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
   Show/Hide
C22H22N4O2S
 1
1 Ki = 21.1 nM
CP0148893
(3S)-N,N-Dimethyl-1-[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]pyrrolidin-3-amine
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C23H24N4O2S
 1
1 Ki = 24.4 nM
CP0017601
2,8-dimethyl-5-[2-(6-methylpyridin-3-yl)ethyl]-3,4-dihydro-1H-pyrido[4,3-b]indole
   Show/Hide
C21H25N3
 2
1 Ki = 26 nM
2 Ki = 34 nM
CP0292029
1-Benzenesulfonyl-3-(2-dimethylamino-ethyl)-1H-indol-5-ol
   Show/Hide
C18H20N2O3S
 1
1 Ki = 28 nM
CP0268549
4-(1,2,3,4-Tetrahydro-carbazole-9-sulfonyl)-phenylamine
   Show/Hide
C18H18N2O2S
 1
1 Ki = 31.62 nM
CP0291340
1-(1-ethylpiperidin-3-yl)-3-[(4-chlorophenyl)sulfonyl]-1H-pyrrolo[2,3-b]pyridine
   Show/Hide
C20H22ClN3O2S
 1
1 Ki = 33.11 nM
CP0073491
(3R)-1-[1-(2-Methylpropyl)-3-(naphthalen-1-ylsulfonyl)-1Hindazol-5-yl]pyrrolidin-3-amine
   Show/Hide
C25H28N4O2S
 1
1 Ki = 36.9 nM
CP0022455
2-Me 5-HT
   Show/Hide
C11H14N2O
 2
1 Ki = 46 nM
2 Ki = 400 nM
CP0043596
(3R)-1-[2-(1-Methylethyl)-3-(naphthalen-1-ylsulfonyl)-2Hindazol-5-yl]pyrrolidin-3-amine
   Show/Hide
C24H26N4O2S
 1
1 Ki = 48.7 nM
CP0034894
2-(5-methoxy-1H-indol-3-yl)ethanamine
   Show/Hide
C11H14N2O
 1
1 Ki < 50 nM
CP0080535
5-fluoro-3-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-1-naphthalen-1-ylsulfonylindole
   Show/Hide
C24H21FN2O2S
 1
1 Ki < 50 nM
CP0099907
6-Chloro-imidazo[2,1-b]thiazole-5-sulfonic acid [1-(2-pyrrolidin-1-yl-ethyl)-1H-indol-6-yl]-amide
   Show/Hide
C19H20ClN5O2S2
 1
1 Ki = 50.12 nM
CP0310112
4-(2,6-dibromopyridin-4-yl)sulfonylaniline
   Show/Hide
C11H8Br2N2O2S
 1
1 Ki = 50.12 nM
CP0330836
(3R)-1-[2-Methyl-3-(naphthalen-1-ylsulfonyl)-2H-indazol-5-yl]pyrrolidin-3-amine
   Show/Hide
C22H22N4O2S
 1
1 Ki = 54.3 nM
CP0036840
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine
   Show/Hide
C14H20N2O
 1
1 Ki = 60 nM
CP0056386
5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one
   Show/Hide
C21H21ClN4OS
 2
1 Ki = 61 nM
2 Ki = 76 nM
CP0069200
1H-indole-3-ethanamine
   Show/Hide
C10H12N2
 1
1 Ki = 70 nM
CP0208161
(3R)-1-[2-(2-Methylpropyl)-3-(naphthalen-1-ylsulfonyl)-2Hindazol-5-yl]pyrrolidin-3-amine
   Show/Hide
C25H28N4O2S
 1
1 Ki = 75.8 nM
CP0277471
N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-nitrobenzenesulfonamide
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C18H22N4O5S
 1
1 Ki = 79.43 nM
CP0087385
2-(5-Methoxy-2-methyl-1H-indol-3-yl)-ethylamine
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C12H16N2O
 1
1 Ki = 80 nM
CP0086335
4-[(2S)-2-[2-[4-(1-benzothiophen-4-yl)piperazin-1-yl]ethyl]pyrrolidin-1-yl]sulfonylisoquinoline
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C27H30N4O2S2
 1
1 Ki = 116 nM
CP0378964
4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonyl-1,3-thiazole
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C20H19ClN2O4S3
 1
1 Ki = 119 nM
CP0359400
(9-Benzyl-6-methoxy-2,3,4,9-tetrahydro-1H-carbazol-4-ylmethyl)-dimethyl-amine
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C23H28N2O
 1
1 Ki = 136 nM
CP0228753
(6-Methoxy-2,3,4,9-tetrahydro-1H-carbazol-4-ylmethyl)-dimethyl-amine
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C16H22N2O
 1
1 Ki = 168 nM
CP0076852
2-(5-methoxy-2-propyl-1H-indol-3-yl)-N,N-dimethylethanamine
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C16H24N2O
 1
1 Ki = 185 nM
CP0042927
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
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C23H27Cl2N3O2
 2
1 Ki = 318 nM
2 Ki > 1000 nM
CP0099712
3-(2-aminoethyl)-1H-indole-5-carboxamide
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C11H13N3O
 1
1 Ki = 720 nM
CP0370109
6-Chloro-imidazo[2,1-b]thiazole-5-sulfonic acid [1-(3-piperidin-1-yl-propyl)-1H-indol-5-yl]-amide
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C21H24ClN5O2S2
 1
1 Ki = 1000 nM
CP0039958
(risperidone)3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one
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C23H27FN4O2
 4
1 Ki = 1190 nM
2 Ki = 1329.2 nM
3 Ki = 2000 nM
4 Ki > 1000 nM
CP0008601
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)
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C21H23ClFNO2
 2
1 Ki = 6000 nM
2 Ki > 5000 nM
CP0370584
4-(2-bromo-6-piperazin-1-ylpyridin-4-yl)sulfonylaniline
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C15H17BrN4O2S
 1
1 Ki ~ 0.1 nM
CP0370117
4-(2-Bromo-6-pyrrolidin-1-yl-pyridine-4-sulfonyl)-phenylamine
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C15H16BrN3O2S
 1
1 Ki ~ 1 nM
CP0096286
(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol
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C18H28N2O3S
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( 5-HT 6 receptor (HTR6) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Schizophrenia [ICD-11: 6A20]
2 Alzheimer disease [ICD-11: 8A20]
3 Neurological disorder [ICD-11: 6B60]
4 Parkinson disease [ICD-11: 8A00.0]
5 Anxiety disorder [ICD-11: 6B00-6B0Z]
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 LU AE58054 Phase 3
Schizophrenia
2 SAM-531 Phase 2
Alzheimer disease
3 SB-742457 Phase 3
Alzheimer disease
4 SUVN-502 Phase 2
Neurological disorder
5 SYN120 Phase 2
Parkinson disease
Discontinued Drug(s) 1 Discontinued Drug  1
1 WAY-181187 Discontinued in Phase 1
Anxiety disorder
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02228 5-hydroxytryptamine receptor 6 Rattus norvegicus, Rat
PT06956 5-hydroxytryptamine receptor 6 Mus musculus, Mouse