Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJS8PY)

• DTT Name: 5-HT 6 receptor (HTR6)
• Synonyms: Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
• Gene Name: HTR6
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT6R_HUMAN
• TTD ID: T16691
• Sequence:
  MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
  SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
  SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
  RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
  RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
  LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
  RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
  FNIDPAEPELRPHPLGIPTN
• Function: The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs. Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity. Is an activator of TOR signaling. 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.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

15 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LU AE58054	DMWGRQD	Schizophrenia	6A20	Phase 3	[2]
SB-742457	DM6L4ZT	Alzheimer disease	8A20	Phase 3	[3]
AVN 211	DMVB4OS	Schizophrenia	6A20	Phase 2/3	[4]
AVN 101	DMJFLBC	Alzheimer disease	8A20	Phase 2	[4]
AVN 322	DMK2LGM	Cognitive impairment	6D71	Phase 2	[3]
PF-05212377	DMPVQYR	Alzheimer disease	8A20	Phase 2	[5]
SAM-531	DMHVJZ6	Alzheimer disease	8A20	Phase 2	[6]
SUVN-502	DMQD753	Alzheimer disease	8A20	Phase 2	[7]
SYN-120	DMPW0UL	Alzheimer disease	8A20	Phase 2	[8]
SYN120	DMDF7XB	Parkinson disease	8A00.0	Phase 2	[9]
11C-GSK-215083	DMQ0RXA	Neurodegenerative disorder	8A20-8A23	Phase 1	[10]
ABT-354	DMWN7D3	Alzheimer disease	8A20	Phase 1	[11]
AVN-322	DMNIVFJ	Alzheimer disease	8A20	Phase 1	[12]
BVT-74316	DMEP321	Obesity	5B81	Phase 1	[13]
PRX-07034	DM5TLAP	Obesity	5B81	Phase 1	[14]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID30124346-Compound-13TABLE4	DMHTJVA	Attention deficit hyperactivity disorder	6A05.Z	Patented	[15]
PMID30124346-Compound-34TABLE4	DM2G3VE	Attention deficit hyperactivity disorder	6A05.Z	Patented	[15]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AVN 397	DMFCOZL	Alzheimer disease	8A20	Discontinued in Phase 2	[4]
SYN-114	DM4JPLM	Cognitive impairment	6D71	Discontinued in Phase 1	[16]
WAY-181187	DM8SVHI	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[17]

105 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[18]
1-(2-Methoxy-phenyl)-piperazine	DM3M4RA	Discovery agent	N.A.	Investigative	[19]
1-(3-(benzyloxy)-2-methylphenyl)piperazine	DMQ4MUF	Discovery agent	N.A.	Investigative	[20]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine	DMX5N3V	Discovery agent	N.A.	Investigative	[21]
1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole	DM7W25U	Discovery agent	N.A.	Investigative	[22]
1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole	DM1N4LK	Discovery agent	N.A.	Investigative	[23]
1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole	DMRA9VG	Discovery agent	N.A.	Investigative	[24]
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[25]
1-phenylthio-N,N-dimethyltryptamine	DM5REQ9	Discovery agent	N.A.	Investigative	[26]
2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine	DM3D8WI	Discovery agent	N.A.	Investigative	[27]
2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine	DMB5LHA	Discovery agent	N.A.	Investigative	[28]
2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine	DMML3XI	Discovery agent	N.A.	Investigative	[28]
2-(1-tosyl-1H-indol-3-yl)ethanamine	DMXCID6	Discovery agent	N.A.	Investigative	[27]
2-(1H-indol-3-yl)-N,N-dimethylethanamine	DMR9Q4Y	Discovery agent	N.A.	Investigative	[29]
2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine	DM94B7N	Discovery agent	N.A.	Investigative	[30]
2-(3-benzenesulfonyl)phenyl-1-aminoethane	DM3FBLT	Discovery agent	N.A.	Investigative	[31]
2-(3-phenylthio)phenyl)-1-aminoethane	DM4WOT6	Discovery agent	N.A.	Investigative	[31]
2-(4-(benzenesulfonyl)phenyl)-1-aminoethane	DMDAO5T	Discovery agent	N.A.	Investigative	[31]
2-Benzyl-4-piperazin-1-yl-1H-benzimidazole	DMYGKW5	Discovery agent	N.A.	Investigative	[32]
2-bromo-LSD	DMOYCWU	Discovery agent	N.A.	Investigative	[25]
2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole	DMLC8OB	Discovery agent	N.A.	Investigative	[33]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[34]
3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole	DMSRHLC	Discovery agent	N.A.	Investigative	[35]
3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole	DM9QB0X	Discovery agent	N.A.	Investigative	[35]
3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole	DMVKO5N	Discovery agent	N.A.	Investigative	[35]
4-((1H-indol-1-yl)methyl)benzenamine	DMRWZ6T	Discovery agent	N.A.	Investigative	[36]
4-(1H-Inden-1-ylmethyl)-phenylamine	DMMJI4R	Discovery agent	N.A.	Investigative	[37]
4-(1H-indol-1-ylsulfonyl)benzenamine	DMY5QBF	Discovery agent	N.A.	Investigative	[22]
4-(1H-Indol-3-ylmethyl)-phenylamine	DMK5CJO	Discovery agent	N.A.	Investigative	[37]
4-(2-benzenesulfonylphenyl)piperazine	DMAZ0LV	Discovery agent	N.A.	Investigative	[31]
4-(3-benzenesulfonamidophenyl)piperazine	DMLVZ6O	Discovery agent	N.A.	Investigative	[31]
4-(3-benzenesulfonylphenyl)piperazine	DMG4X13	Discovery agent	N.A.	Investigative	[31]
4-(3-Methyl-indole-1-sulfonyl)-phenylamine	DM67A4U	Discovery agent	N.A.	Investigative	[19]
4-(3H-Inden-1-ylmethyl)-phenylamine	DM3QJVT	Discovery agent	N.A.	Investigative	[37]
4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine	DMI1598	Discovery agent	N.A.	Investigative	[22]
4-(4-benzenesulfonamidophenyl)piperazine	DMP0G1W	Discovery agent	N.A.	Investigative	[31]
4-(4-benzenesulfonylphenyl)piperazine	DM0DZFX	Discovery agent	N.A.	Investigative	[31]
4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine	DMA7LEO	Discovery agent	N.A.	Investigative	[38]
4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine	DM3L5I6	Discovery agent	N.A.	Investigative	[38]
4-(Indan-1-ylsulfanyl)-phenylamine	DMHI50W	Discovery agent	N.A.	Investigative	[37]
4-(Indane-1-sulfonyl)-phenylamine	DM201UM	Discovery agent	N.A.	Investigative	[37]
4-(Naphthalene-1-sulfonyl)-phenylamine	DMI5XB1	Discovery agent	N.A.	Investigative	[19]
4-(piperazin-1-yl)-1H-indole	DMM1RCS	Discovery agent	N.A.	Investigative	[22]
4-(piperazin-1-yl)-3-tosyl-1H-indazole	DM1HM3F	Discovery agent	N.A.	Investigative	[39]
4-Indan-1-ylmethyl-phenylamine	DM6YON7	Discovery agent	N.A.	Investigative	[37]
4-Inden-(1E)-ylidenemethyl-phenylamine	DM23E0R	Discovery agent	N.A.	Investigative	[37]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[40]
5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole	DMNSIF2	Discovery agent	N.A.	Investigative	[39]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[41]
5-MEO-DMT	DMG0EL7	Discovery agent	N.A.	Investigative	[42]
5-METHOXYTRYPTAMINE	DMARCKD	Discovery agent	N.A.	Investigative	[43]
6-(piperazin-1-yl)-3-tosyl-1H-indazole	DMM9G0J	Discovery agent	N.A.	Investigative	[39]
6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole	DMVL218	Discovery agent	N.A.	Investigative	[44]
alpha-ergocryptine	DMMPOEK	Discovery agent	N.A.	Investigative	[45]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[45]
AMR-SIX-1	DM7WTKJ	Obesity	5B81	Investigative	[46]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[47]
bufotenine	DMD1SY9	Discovery agent	N.A.	Investigative	[34]
CHLOROPHENYLPIPERAZINE	DMOA8L2	Discovery agent	N.A.	Investigative	[48]
DIMEBOLIN	DMV8ZQG	Discovery agent	N.A.	Investigative	[49]
DM-1451	DMM0VDK	Discovery agent	N.A.	Investigative	[50]
E-6837	DMJ2P0N	Discovery agent	N.A.	Investigative	[28]
E6801	DM7LGAF	Discovery agent	N.A.	Investigative	[43]
EDMT	DMS3AXK	Discovery agent	N.A.	Investigative	[51]
EMD-386088	DM3AGUQ	Discovery agent	N.A.	Investigative	[33]
fluperlapine	DM9KIPU	Discovery agent	N.A.	Investigative	[52]
lergotrile	DMDV67S	Discovery agent	N.A.	Investigative	[25]
LY 165,163	DM9IU21	Discovery agent	N.A.	Investigative	[25]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[25]
METHIOTHEPIN	DMMC0I7	Discovery agent	N.A.	Investigative	[53]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[51]
N,N-diethyl-2-(1H-indol-3-yl)ethanamine	DM0UBI9	Discovery agent	N.A.	Investigative	[42]
N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine	DMYUQDK	Discovery agent	N.A.	Investigative	[36]
N-(3-(2-aminoethyl)phenyl)benzenesulfonamide	DMP8547	Discovery agent	N.A.	Investigative	[31]
N-(3-(3-aminopropyl)phenyl)benzenesulfonamide	DMW59AY	Discovery agent	N.A.	Investigative	[31]
N-(3-(aminomethyl)phenyl)benzenesulfonamide	DMSC862	Discovery agent	N.A.	Investigative	[31]
N-(3-aminophenyl)benzenesulfonamide	DMJ6FP7	Discovery agent	N.A.	Investigative	[31]
N-(4-(2-aminoethyl)phenyl)benzenesulfonamide	DM1V83P	Discovery agent	N.A.	Investigative	[31]
N-phenyl-3-(2-aminoethyl)benzenesulfonamide	DMWH86J	Discovery agent	N.A.	Investigative	[31]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[43]
OPC 4392	DMQOJY2	Discovery agent	N.A.	Investigative	[50]
QUIPAZINE	DMPY6IG	Discovery agent	N.A.	Investigative	[48]
Ro-04-6790	DM6H8JM	Discovery agent	N.A.	Investigative	[28]
SB 258585	DM2QJKZ	Discovery agent	N.A.	Investigative	[54]
SB-214111	DMH1CFX	Discovery agent	N.A.	Investigative	[55]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[20]
SB-357134	DMFTO8R	Discovery agent	N.A.	Investigative	[56]
SB399885	DMFMK89	Discovery agent	N.A.	Investigative	[57]
SEL-73	DMFKE6C	Psychiatric disorder	6E8Z	Investigative	[46]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[53]
SUVN-501	DMT8PKC	Neurological disorder	6B60	Investigative	[46]
SUVN-504	DMZCKDH	Vomiting	MD90	Investigative	[46]
SUVN-507	DM2UMK8	Neurological disorder	6B60	Investigative	[46]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[25]
WAY-208466	DM9K2LU	Discovery agent	N.A.	Investigative	[30]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[58]
[125I]SB-258585	DMXWZCB	Discovery agent	N.A.	Investigative	[54]
[2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine	DMAJCVL	Discovery agent	N.A.	Investigative	[37]
[2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine	DMU5P8O	Discovery agent	N.A.	Investigative	[59]
[2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine	DMBTRN6	Discovery agent	N.A.	Investigative	[37]
[2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine	DM1RW4U	Discovery agent	N.A.	Investigative	[59]
[3H]5-CT	DMEAHFZ	Discovery agent	N.A.	Investigative	[46]
[3H]LSD	DM0YJHS	Discovery agent	N.A.	Investigative	[50]
[3H]Ro 63-0563	DM5XSMN	Discovery agent	N.A.	Investigative	[1]
[3H]spiperone	DMWHEV8	Discovery agent	N.A.	Investigative	[48]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Schizophrenia	6A20	Pre-frontal cortex	6.43E-01	0.04	0.12
Schizophrenia	6A20	Superior temporal cortex	3.59E-02	-0.05	-0.48
Alzheimer's disease	8A00.0	Entorhinal cortex	1.23E-05	-0.12	-0.71

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