Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT0WAIE)

• DTT Name: Melatonin receptor type 1A (MTNR1A)
• Synonyms: Mel1a receptor; Mel1AR; Mel-1A-R
• Gene Name: MTNR1A
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: MTR1A_HUMAN
• TTD ID: T97613
• Sequence:
  MQGNGSALPNASQPVLRGDGARPSWLASALACVLIFTIVVDILGNLLVILSVYRNKKLRN
  AGNIFVVSLAVADLVVAIYPYPLVLMSIFNNGWNLGYLHCQVSGFLMGLSVIGSIFNITG
  IAINRYCYICHSLKYDKLYSSKNSLCYVLLIWLLTLAAVLPNLRAGTLQYDPRIYSCTFA
  QSVSSAYTIAVVVFHFLVPMIIVIFCYLRIWILVLQVRQRVKPDRKPKLKPQDFRNFVTM
  FVVFVLFAICWAPLNFIGLAVASDPASMVPRIPEWLFVASYYMAYFNSCLNAIIYGLLNQ
  NFRKEYRRIIVSLCTARVFFVDSSNDVADRVKWKPSPLMTNNNVVKVDSV
• Function: Likely to mediate the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity. High affinity receptor for melatonin.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Circadian entrainment (hsa04713)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Melatonin	DMKWFBT	Depression	6A70-6A7Z	Approved	[1]
Ramelteon	DM7IW9J	Insomnia	7A00-7A0Z	Approved	[2]
Tasimelteon	DMLOQ1V	Insomnia	7A00-7A0Z	Approved	[3]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY-156735	DM5IX9M	Anxiety disorder	6B00-6B0Z	Phase 2	[4]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[5]

6 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Agomelatine	DMXYA5K	Major depressive disorder	6A70.3	Withdrawn from market	[6]
GR-131663	DMKAGLV	Anxiety disorder	6B00-6B0Z	Terminated	[7]
GR-133347	DMNRJA0	Anxiety disorder	6B00-6B0Z	Terminated	[8]
Luzindole	DMXRJQV	Sleep-wake disorder	7A00-7B2Z	Terminated	[9]
S-20928	DMQDWMJ	Sleep-wake disorder	7A00-7B2Z	Terminated	[10]
SL-18.1616	DMI1WNF	Insomnia	7A00-7A0Z	Terminated	[11]

51 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(hydroxymethylphenyl)agomelatine	DMOJUEC	Discovery agent	N.A.	Investigative	[12]
2-(indolin-1yl)-melatonin	DMOVYXT	Discovery agent	N.A.	Investigative	[13]
2-iodo-melatonin	DMSEIUP	Discovery agent	N.A.	Investigative	[14]
2-methoxy-alpha,beta-didehydro-agomelatine	DM4G3FS	Discovery agent	N.A.	Investigative	[15]
2-[125I]melatonin	DMFJOHG	Discovery agent	N.A.	Investigative	[16]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[17]
4P-PDOT	DMEMN0W	Discovery agent	N.A.	Investigative	[18]
5-HEAT	DMKUT6A	Discovery agent	N.A.	Investigative	[19]
5-methoxy-luzindole	DMUXTWC	Discovery agent	N.A.	Investigative	[16]
5-methoxycarbonylamino-N-acetyltryptamine	DMCZSP3	Discovery agent	N.A.	Investigative	[20]
6-Cl-MLT	DMKNOLV	Discovery agent	N.A.	Investigative	[14]
6-hydroxymelatonin	DM89YV7	Discovery agent	N.A.	Investigative	[14]
AAE-M-PBP-amine	DMNO51B	Discovery agent	N.A.	Investigative	[21]
Beta,beta-dimethylmelatonin	DM6FHQD	Discovery agent	N.A.	Investigative	[22]
Beta-methylmelatonin	DMKH32S	Discovery agent	N.A.	Investigative	[22]
BOMPPA	DMI75A3	Discovery agent	N.A.	Investigative	[23]
CBOBNEA	DMITY0H	Discovery agent	N.A.	Investigative	[24]
CIFEA	DMP35OM	Discovery agent	N.A.	Investigative	[25]
DH97	DM7UVOD	Discovery agent	N.A.	Investigative	[26]
difluoroagomelatine	DM8AZQ3	Discovery agent	N.A.	Investigative	[27]
EFPPEA	DMZ2XOH	Discovery agent	N.A.	Investigative	[28]
GR 128107	DMAI9Y0	Discovery agent	N.A.	Investigative	[29]
GR 196429	DMHAWYJ	Discovery agent	N.A.	Investigative	[30]
IIK7	DMLYIBO	Discovery agent	N.A.	Investigative	[31]
isoamyl-agomelatine	DMGNFXY	Discovery agent	N.A.	Investigative	[27]
K185	DME65H8	Discovery agent	N.A.	Investigative	[31]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide	DMWC70I	Discovery agent	N.A.	Investigative	[32]
N-(2,3-Dihydro-1H-phenalen-2-yl)-acetamide	DMPL26K	Discovery agent	N.A.	Investigative	[33]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide	DM4V7AS	Discovery agent	N.A.	Investigative	[20]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide	DM4ZTF1	Discovery agent	N.A.	Investigative	[34]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide	DMLWGPC	Discovery agent	N.A.	Investigative	[34]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide	DMI452E	Discovery agent	N.A.	Investigative	[34]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide	DMH0LOT	Discovery agent	N.A.	Investigative	[13]
N-(3-(3-methoxyphenyl)propyl)acetamide	DMSZ03N	Discovery agent	N.A.	Investigative	[34]
N-(3-(3-methoxyphenyl)propyl)propionamide	DMKSM5A	Discovery agent	N.A.	Investigative	[34]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide	DMILWPS	Discovery agent	N.A.	Investigative	[34]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide	DMHM0WI	Discovery agent	N.A.	Investigative	[34]
N-acetylserotonin	DMJ4SBM	Discovery agent	N.A.	Investigative	[33]
S22153	DM4S5TQ	Discovery agent	N.A.	Investigative	[35]
S24014	DM9RU46	Discovery agent	N.A.	Investigative	[35]
S24773	DM1HAD0	Discovery agent	N.A.	Investigative	[35]
S26131	DMCJ86U	Discovery agent	N.A.	Investigative	[35]
S26284	DMLJITC	Discovery agent	N.A.	Investigative	[35]
UCM 549	DM9JG1L	Discovery agent	N.A.	Investigative	[36]
UCM 724	DMCKSYQ	Discovery agent	N.A.	Investigative	[36]
UCM 765	DMD16MH	Discovery agent	N.A.	Investigative	[37]
UCM 793	DM8J41W	Discovery agent	N.A.	Investigative	[37]
UCM-454	DMSVJFG	Discovery agent	N.A.	Investigative	[13]
[125I]DIV880	DMEPT8H	Discovery agent	N.A.	Investigative	[38]
[125I]S70254	DMHC6KX	Discovery agent	N.A.	Investigative	[38]
[125I]SD6	DM285MQ	Discovery agent	N.A.	Investigative	[38]

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	5.71E-01	-0.08	-0.54

References

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