Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTWJBZ5)

• DTT Name: 5-HT 2C receptor (HTR2C)
• Synonyms: Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
• Gene Name: HTR2C
• DTT Type: Successful target; [1]
• Related Disease:
  Depression [ICD-11: 6A70-6A7Z]
  Migraine [ICD-11: 8A80]
  Obesity [ICD-11: 5B80-5B81]
  Pain [ICD-11: MG30-MG3Z]
  Pituitary gland disorder [ICD-11: 5A60-5A61]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT2C_HUMAN
• TTD ID: T83813
• Sequence:
  MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
  VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
  PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
  ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
  LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
  QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
  SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
  EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
• Function: Functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Gap junction (hsa04540)
  Serotonergic synapse (hsa04726)
  Inflammatory mediator regulation of TRP channels (hsa04750)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

6 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[2], [3]
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[4]
Methysergide	DM1EF73	Migraine	8A80	Approved	[1], [5], [6], [7]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[8], [9]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[9], [10]
Tramadol	DMRQD04	Pain	MG30-MG3Z	Approved	[11]

9 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[12]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[13]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[14]
ATHX-105	DM6ABD9	Obesity	5B81	Phase 2	[15]
Nuplazid	DMOJA5G	Alzheimer disease	8A20	Phase 2	[16]
PRX00933	DM1JNDV	Diabetic complication	5A2Y	Phase 2	[17]
Puerarin	DMJIMXH	Alcohol dependence	6C40.2	Phase 2	[18]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[19], [20]
Tedatioxetine	DMV5LGJ	Generalized anxiety disorder	6B00	Phase 1	[21]

39 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aryl piperazine derivative 10	DM5EGBY	N. A.	N. A.	Patented	[22]
Aryl piperazine derivative 8	DM7BRIT	N. A.	N. A.	Patented	[22]
Aryl piperazine derivative 9	DMLKNWF	N. A.	N. A.	Patented	[22]
Benzazepine derivative 1	DMA3BCU	N. A.	N. A.	Patented	[22]
Benzazepine derivative 2	DMKREJ2	N. A.	N. A.	Patented	[22]
Benzazepine derivative 3	DM3BGEN	N. A.	N. A.	Patented	[22]
Benzazepine derivative 4	DMM72LS	N. A.	N. A.	Patented	[22]
Benzazepine derivative 5	DM6XRDH	N. A.	N. A.	Patented	[22]
Benzazepine derivative 6	DMCGX5S	N. A.	N. A.	Patented	[22]
Chromene derivative 1	DM7SOZN	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 1	DMDOQKY	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 10	DMMZ8LE	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 11	DM5BF6H	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 12	DMOG72B	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 13	DME86DP	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 14	DMG1TIF	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 15	DMS3WEJ	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 2	DMDFL6B	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 3	DMG14E3	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 4	DMZVLH2	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 5	DMON5RD	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 6	DM3O7UG	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 7	DMS6HOG	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 8	DMBJH8N	N. A.	N. A.	Patented	[22]
Heteroaryl-azepine derivative 9	DMUZR3X	N. A.	N. A.	Patented	[22]
PMID26609882-Compound-58	DMD3T1Q	N. A.	N. A.	Patented	[22]
PMID26609882-Compound-83	DM6C45G	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 23	DM5MLQU	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 24	DMOQ726	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 25	DM51MFS	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 26	DM90WKN	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 27	DMIQSDW	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 28	DM1D2AS	N. A.	N. A.	Patented	[22]
Pyrimidine derivative 29	DMVOYJ8	N. A.	N. A.	Patented	[22]
Quinoline derivative 2	DMNO2BP	N. A.	N. A.	Patented	[22]
Tricyclic pyrrolidine derivative 1	DMGY3OR	N. A.	N. A.	Patented	[22]
Tricyclic pyrrolidine derivative 2	DMRD1XJ	N. A.	N. A.	Patented	[22]
Tricyclic pyrrolidine derivative 3	DMK2V6H	N. A.	N. A.	Patented	[22]
Tricyclic pyrrolidine derivative 4	DM0JYWT	N. A.	N. A.	Patented	[22]

10 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Deramciclane	DM8DUZT	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[23], [24], [25]
Ritanserin	DM0X36Y	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[26], [27], [28], [29]
MCPP	DMIG5W8	Mood disorder	6A60-6E23	Discontinued in Phase 2	[30], [31]
R-1065	DMHPV1D	Obesity	5B81	Discontinued in Phase 1	[32]
SB-247853	DMOVLDT	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[33], [31]
ICI-169369	DMQ0IOF	Anxiety disorder	6B00-6B0Z	Terminated	[34]
LY53857	DMY71LJ	N. A.	N. A.	Terminated	[35], [36], [37], [7]
Org-37684	DMY3LXH	Anxiety disorder	6B00-6B0Z	Terminated	[38]
Ro-60-0175	DMZSQU8	N. A.	N. A.	Terminated	[39]
SDZ-SER-082	DMXHW91	Neurological disorder	6B60	Terminated	[40]

107 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[41]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine	DMIS39C	Discovery agent	N.A.	Investigative	[39]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine	DMW4ARM	Discovery agent	N.A.	Investigative	[39]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine	DM31SNW	Discovery agent	N.A.	Investigative	[39]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine	DMYALON	Discovery agent	N.A.	Investigative	[39]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine	DMTJI4F	Discovery agent	N.A.	Investigative	[42]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine	DMKZ4C6	Discovery agent	N.A.	Investigative	[43]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine	DMTZDAJ	Discovery agent	N.A.	Investigative	[43]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine	DMAU1M5	Discovery agent	N.A.	Investigative	[43]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine	DMS2DI9	Discovery agent	N.A.	Investigative	[43]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine	DM0YELX	Discovery agent	N.A.	Investigative	[43]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine	DMEIB8F	Discovery agent	N.A.	Investigative	[43]
1-((R)-2-aminopropyl)-1H-indazol-6-ol	DM74R0E	Discovery agent	N.A.	Investigative	[44]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[44]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol	DMRFJNC	Discovery agent	N.A.	Investigative	[44]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol	DM76JVB	Discovery agent	N.A.	Investigative	[44]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol	DMR2SXL	Discovery agent	N.A.	Investigative	[44]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol	DM8MNZG	Discovery agent	N.A.	Investigative	[44]
1-(2-aminoethyl)-1H-indazol-6-ol	DMKWO6A	Discovery agent	N.A.	Investigative	[44]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol	DMM3LET	Discovery agent	N.A.	Investigative	[45]
1-(piperazin-1-yl)isoquinoline	DMEP80C	Discovery agent	N.A.	Investigative	[46]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol	DMO7NXE	Discovery agent	N.A.	Investigative	[45]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine	DM1O0JD	Discovery agent	N.A.	Investigative	[44]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline	DML6HSE	Discovery agent	N.A.	Investigative	[46]
3-(2-Amino-propyl)-1H-indol-5-ol	DMQPNUM	Discovery agent	N.A.	Investigative	[44]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol	DMKYZGD	Discovery agent	N.A.	Investigative	[45]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol	DM32MIE	Discovery agent	N.A.	Investigative	[45]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol	DM9BTLC	Discovery agent	N.A.	Investigative	[45]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol	DMMJP9D	Discovery agent	N.A.	Investigative	[45]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol	DM7VJPX	Discovery agent	N.A.	Investigative	[45]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol	DM0O2ZB	Discovery agent	N.A.	Investigative	[45]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol	DMDOIJM	Discovery agent	N.A.	Investigative	[45]
3-Dimethylaminomethyl-1H-indol-4-ol	DMSJUOH	Discovery agent	N.A.	Investigative	[45]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[47]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine	DMTNVFZ	Discovery agent	N.A.	Investigative	[46]
4-(piperazin-1-yl)furo[3,2-c]pyridine	DMNM8VY	Discovery agent	N.A.	Investigative	[46]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine	DMNU2RM	Discovery agent	N.A.	Investigative	[46]
4-(piperazin-1-yl)thieno[3,2-c]pyridine	DMJGTS7	Discovery agent	N.A.	Investigative	[46]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine	DM2KAG5	Discovery agent	N.A.	Investigative	[46]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[48]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[48]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine	DMGDTNI	Discovery agent	N.A.	Investigative	[48]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine	DM7FZU2	Discovery agent	N.A.	Investigative	[48]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide	DMZ5MDY	Discovery agent	N.A.	Investigative	[43]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[49]
5-MEO-DMT	DMG0EL7	Discovery agent	N.A.	Investigative	[44]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine	DM592FB	Discovery agent	N.A.	Investigative	[50]
6-(piperazin-1-yl)-9-propyl-9H-purine	DMUNWJR	Discovery agent	N.A.	Investigative	[46]
6-bromo-2'-de-N-methylaplysinopsin	DM39VT6	Discovery agent	N.A.	Investigative	[51]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine	DMZJ6M8	Discovery agent	N.A.	Investigative	[46]
6-bromoaplysinopsin	DMQGB70	Discovery agent	N.A.	Investigative	[51]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide	DMUY9TF	Discovery agent	N.A.	Investigative	[43]
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine	DM1LW62	Discovery agent	N.A.	Investigative	[46]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine	DMIMLUO	Discovery agent	N.A.	Investigative	[50]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine	DMVZA27	Discovery agent	N.A.	Investigative	[50]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine	DMK6U2V	Discovery agent	N.A.	Investigative	[48]
AL-37350A	DMRJ2GK	Discovery agent	N.A.	Investigative	[52]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[53]
Aplysinopsin	DMUPL3J	Discovery agent	N.A.	Investigative	[43]
BARETTIN	DMU3D2O	Discovery agent	N.A.	Investigative	[54]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[55]
BVT 933	DM8N7BA	Obesity	5B81	Investigative	[56]
BW723C86	DME15JU	Discovery agent	N.A.	Investigative	[57]
Chlorophenylpiperazine	DMOA8L2	Discovery agent	N.A.	Investigative	[58]
CP-809101	DM3M1LA	Neurological disorder	6B60	Investigative	[59]
CSC-500297	DM6K123	Obesity	5B81	Investigative	[59]
Cyamemazine	DMZ6YPV	Discovery agent	N.A.	Investigative	[60]
Cyclo[(6-bromotryptophan)arginine]	DM9ZCWV	Discovery agent	N.A.	Investigative	[54]
EGIS-7625	DMLK4X5	Discovery agent	N.A.	Investigative	[61]
FR260010	DMSQ6CV	Discovery agent	N.A.	Investigative	[62]
LY334362	DMFHT3U	Discovery agent	N.A.	Investigative	[63]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[64]
Methylenedioxymethamphetamine	DMYVU47	Discovery agent	N.A.	Investigative	[65]
MK-212	DMYO8T6	Discovery agent	N.A.	Investigative	[66], [67]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[68]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide	DM2E5OX	Discovery agent	N.A.	Investigative	[69]
N-(pyridin-3-yl)indoline-1-carboxamide	DMTHJL4	Discovery agent	N.A.	Investigative	[43]
N-3'-ethylaplysinopsin	DMWZTKD	Discovery agent	N.A.	Investigative	[51]
norfluoxetine	DMKNUP3	Discovery agent	N.A.	Investigative	[70]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[71]
Org 12962	DM8JUBG	Discovery agent	N.A.	Investigative	[4]
PG-01037	DM2TP4Q	Discovery agent	N.A.	Investigative	[72]
RS-102,221	DMHDYBN	Discovery agent	N.A.	Investigative	[73]
SB 204741	DM3LQF4	Discovery agent	N.A.	Investigative	[4]
SB 215505	DMCM4LT	Discovery agent	N.A.	Investigative	[74]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[55]
SB 221284	DM8DVY2	Discovery agent	N.A.	Investigative	[4]
SB 228357	DMKA8R4	Discovery agent	N.A.	Investigative	[75]
SB 242084	DMISBDC	Discovery agent	N.A.	Investigative	[76]
SB 243213	DMAFWRT	Discovery agent	N.A.	Investigative	[77]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[78]
Serotonin	DMOFCRY	Discovery agent	N.A.	Investigative	[54]
spiramide	DM5KNMD	Discovery agent	N.A.	Investigative	[4]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[49]
TQ-1017	DMEF32D	Pain	MG30-MG3Z	Investigative	[31]
VER-2692	DM5WAM8	Discovery agent	N.A.	Investigative	[79]
VER-3323	DM7O2K1	Discovery agent	N.A.	Investigative	[80]
VER-5384	DMC2EO9	Discovery agent	N.A.	Investigative	[80]
VER-5593	DMZ2V0A	Discovery agent	N.A.	Investigative	[80]
WAY-163909	DMNMO4Q	Discovery agent	N.A.	Investigative	[81]
WAY-208466	DM9K2LU	Discovery agent	N.A.	Investigative	[82]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[83]
YM-348	DM38F9T	Discovery agent	N.A.	Investigative	[50]
[125I]DOI	DMQUY08	Discovery agent	N.A.	Investigative	[53]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMDIH96	Discovery agent	N.A.	Investigative	[45]
[3H]LSD	DM0YJHS	Discovery agent	N.A.	Investigative	[59]
[3H]mesulergine	DM8K6VF	Discovery agent	N.A.	Investigative	[53]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Schizophrenia	6A20	Pre-frontal cortex	1.02E-02	-0.45	-0.37
Schizophrenia	6A20	Superior temporal cortex	2.27E-01	0.27	0.6
Major depressive disorder	6A20	Pre-frontal cortex	8.66E-01	-0.13	-0.12

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