Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT6MSOK)

• DTT Name: 5-HT 1D receptor (HTR1D)
• Synonyms: Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
• Gene Name: HTR1D
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT1D_HUMAN
• TTD ID: T11072
• Sequence:
  MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
  TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
  CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
  AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
  TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
  KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
  EEFRQAFQKIVPFRKAS
• Function: Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

7 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Almogran	DM7I64Z	Migraine	8A80	Approved	[2]
Eletriptan	DMW649X	Migraine	8A80	Approved	[3]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[3]
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[4]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[5]
Sumatriptan	DMVYXR8	Cluster headache	8A81.0	Approved	[1]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[3]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[6]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[7]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[8]
TGBA01AD	DMJ2FTU	Mood disorder	6A60-6E23	Phase 2	[9]
Tonabersat	DMT4OPL	Epilepsy	8A60-8A68	Phase 2	[10]

16 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alniditan	DMFE3CT	Migraine	8A80	Discontinued in Phase 3	[11]
Avitriptan	DM3SE2N	Migraine	8A80	Discontinued in Phase 3	[12]
BMS-181101	DMT4VSE	Mood disorder	6A60-6E23	Discontinued in Phase 2	[13]
CP-122288	DM3OJP0	Migraine	8A80	Discontinued in Phase 2	[14]
Elzasonan hydrochloride	DM1EOC3	Mood disorder	6A60-6E23	Discontinued in Phase 2	[15]
IS-159	DMLQWFA	Migraine	8A80	Discontinued in Phase 2	[16]
PNU-142633	DMLK5IM	Migraine	8A80	Discontinued in Phase 2	[17]
ALX-0646	DMNOZAI	Migraine	8A80	Discontinued in Phase 1	[18]
Tidembersat	DMTC4LP	Migraine	8A80	Discontinued in Phase 1	[18]
BMS-181885	DMYWI04	Migraine	8A80	Terminated	[13]
GR-127935	DM01HLX	Major depressive disorder	6A70.3	Terminated	[20]
L-694247	DM2F4GT	Migraine	8A80	Terminated	[21]
L-741604	DMNSH0V	N. A.	N. A.	Terminated	[22]
L-775606	DMJ37IX	N. A.	N. A.	Terminated	[23]
PNU-109291	DMZNM2K	Migraine	8A80	Terminated	[24]
VR-147	DMLWQOP	Migraine	8A80	Terminated	[25]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Donitriptan	DMA2K7C	Migraine	8A80	Preclinical	[19]

78 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[26]
(3-Chloro-phenyl)-piperazin-1-yl-methanone	DM7U02R	Discovery agent	N.A.	Investigative	[27]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine	DMP4DLV	Discovery agent	N.A.	Investigative	[28]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[29]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine	DM31CVR	Discovery agent	N.A.	Investigative	[27]
1-(2,5-Dimethoxy-phenyl)-piperazine	DMNETHQ	Discovery agent	N.A.	Investigative	[27]
1-(2,5-dimethoxyphenyl)propan-2-amine	DM043N8	Discovery agent	N.A.	Investigative	[30]
1-(2-Butoxy-phenyl)-piperazine	DMT5S2O	Discovery agent	N.A.	Investigative	[31]
1-(2-Ethoxy-phenyl)-piperazine	DM2P7YX	Discovery agent	N.A.	Investigative	[31]
1-(2-Fluoro-phenyl)-piperazine	DM94LID	Discovery agent	N.A.	Investigative	[31]
1-(2-Isopropoxy-phenyl)-piperazine	DM5KAH6	Discovery agent	N.A.	Investigative	[31]
1-(2-Methoxy-phenyl)-piperazine	DM3M4RA	Discovery agent	N.A.	Investigative	[31]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine	DMX5N3V	Discovery agent	N.A.	Investigative	[32]
1-(3-Fluoro-phenyl)-piperazine	DM2SNR0	Discovery agent	N.A.	Investigative	[31]
1-(3-Nitro-phenyl)-piperazine	DMMJC5E	Discovery agent	N.A.	Investigative	[31]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine	DMCH6R1	Discovery agent	N.A.	Investigative	[27]
1-(7-Methoxy-naphthalen-2-yl)-piperazine	DM1MJCE	Discovery agent	N.A.	Investigative	[33]
1-Naphthalen-2-yl-piperazine	DMJK0MF	Discovery agent	N.A.	Investigative	[28]
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[34]
2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole	DM7JUK0	Discovery agent	N.A.	Investigative	[35]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol	DMZNRFG	Discovery agent	N.A.	Investigative	[30]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine	DMDI98B	Discovery agent	N.A.	Investigative	[30]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine	DM4C9H2	Discovery agent	N.A.	Investigative	[30]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine	DM79JVK	Discovery agent	N.A.	Investigative	[30]
2-(4-Bromo-phenyl)-1-methyl-ethylamine	DMB49UP	Discovery agent	N.A.	Investigative	[30]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole	DM1A4BS	Discovery agent	N.A.	Investigative	[35]
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine	DM2TU6W	Discovery agent	N.A.	Investigative	[36]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine	DM1AEK4	Discovery agent	N.A.	Investigative	[37]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[38]
2-Piperazin-1-yl-benzonitrile	DM742IJ	Discovery agent	N.A.	Investigative	[31]
2-Piperazin-1-yl-phenol	DMQT9OK	Discovery agent	N.A.	Investigative	[27]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one	DMKGIQ1	Discovery agent	N.A.	Investigative	[27]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[39]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole	DMJKQ5I	Discovery agent	N.A.	Investigative	[23]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[39]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine	DM7FZU2	Discovery agent	N.A.	Investigative	[39]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[4]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMK57W2	Discovery agent	N.A.	Investigative	[40]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMXGRMB	Discovery agent	N.A.	Investigative	[40]
7-methoxy-1-naphthylpiperazine	DM3MXI5	Discovery agent	N.A.	Investigative	[33]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline	DMQIFZC	Discovery agent	N.A.	Investigative	[28]
8-Methoxy-2-piperazin-1-yl-quinoline	DMNWC29	Discovery agent	N.A.	Investigative	[28]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine	DMK6U2V	Discovery agent	N.A.	Investigative	[39]
8-Methoxy-quinolin-2-ylamine	DMHZ5SB	Discovery agent	N.A.	Investigative	[28]
9-OH-risperidone	DMGORXQ	Discovery agent	N.A.	Investigative	[41]
AGROCLAVINE	DMT9FJZ	Discovery agent	N.A.	Investigative	[42]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[38]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[43]
Brolamfetamine	DMC4PF0	Discovery agent	N.A.	Investigative	[30]
bufotenine	DMD1SY9	Discovery agent	N.A.	Investigative	[38]
CHLOROPHENYLPIPERAZINE	DMOA8L2	Discovery agent	N.A.	Investigative	[31]
dipropyl-5-CT	DM9VKXC	Discovery agent	N.A.	Investigative	[34]
EDMT	DMS3AXK	Discovery agent	N.A.	Investigative	[44]
Etisulergine	DMKH8TC	Discovery agent	N.A.	Investigative	[45]
L-747201	DMBPWSJ	Discovery agent	N.A.	Investigative	[46]
L-760790	DMA9VDN	Discovery agent	N.A.	Investigative	[22]
L-772,405	DM5O0CM	Discovery agent	N.A.	Investigative	[47]
lysergic acid	DM4MGAQ	Discovery agent	N.A.	Investigative	[38]
lysergol	DM1OHF8	Discovery agent	N.A.	Investigative	[34]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[4]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[44]
PHENYLPIPERAZINE	DMWAK1R	Discovery agent	N.A.	Investigative	[28]
QUIPAZINE	DMPY6IG	Discovery agent	N.A.	Investigative	[28]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[43]
SB 272183	DMOLNQX	Discovery agent	N.A.	Investigative	[48]
SB 649915	DM21Z6H	Discovery agent	N.A.	Investigative	[49]
SB 714786	DMGHRY0	Discovery agent	N.A.	Investigative	[49]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[23]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[4]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[50]
[125I]GTI	DMSYT5P	Discovery agent	N.A.	Investigative	[51]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMOZ73L	Discovery agent	N.A.	Investigative	[40]
[3H]5-CT	DMEAHFZ	Discovery agent	N.A.	Investigative	[52]
[3H]5-HT	DMYJXV7	Discovery agent	N.A.	Investigative	[11]
[3H]8-OH-DPAT	DM4KCYU	Discovery agent	N.A.	Investigative	[53]
[3H]eletriptan	DMDTYRV	Discovery agent	N.A.	Investigative	[54]
[3H]GR 125,743	DM4URBO	Discovery agent	N.A.	Investigative	[52]
[3H]sumatriptan	DM3MBGV	Discovery agent	N.A.	Investigative	[54]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Major depressive disorder	6A20	Pre-frontal cortex	4.57E-01	-0.02	-0.15

References

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