Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Dopamine D1 receptor (D1R)
• Synonyms: D(1A) dopamine receptor
• Gene Name: DRD1
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: DRD1_HUMAN
• TTD ID: T22118
• Sequence:
  MRTLNTSAMDGTGLVVERDFSVRILTACFLSLLILSTLLGNTLVCAAVIRFRHLRSKVTN
  FFVISLAVSDLLVAVLVMPWKAVAEIAGFWPFGSFCNIWVAFDIMCSTASILNLCVISVD
  RYWAISSPFRYERKMTPKAAFILISVAWTLSVLISFIPVQLSWHKAKPTSPSDGNATSLA
  ETIDNCDSSLSRTYAISSSVISFYIPVAIMIVTYTRIYRIAQKQIRRIAALERAAVHAKN
  CQTTTGNGKPVECSQPESSFKMSFKRETKVLKTLSVIMGVFVCCWLPFFILNCILPFCGS
  GETQPFCIDSNTFDVFVWFGWANSSLNPIIYAFNADFRKAFSTLLGCYRLCPATNNAIET
  VSINNNGAAMFSSHHEPRGSISKECNLVYLIPHAVGSSEDLKKEEAAGIARPLEKLSPAL
  SVILDYDTDVSLEKIQPITQNGQHPT
• Function: Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Gap junction (hsa04540)
  Dopaminergic synapse (hsa04728)
  Parkinson's disease (hsa05012)
  Cocaine addiction (hsa05030)
  Amphetamine addiction (hsa05031)
  Morphine addiction (hsa05032)
  Alcoholism (hsa05034)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Dopamine receptors (R-HSA-390651)

Molecular Interaction Atlas (MIA) of This DTT

4 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fenoldopam	DMFAOKP	Hypertension	BA00-BA04	Approved	[1]
Methylergonovine	DMBEX4O	Spontaneous abortion	JA00.0	Approved	[2]
Pergolide	DM14MAE	Parkinson disease	8A00.0	Approved	[3]
Phenyltoloxamine	DMKAEQW	Allergy	4A80-4A85	Approved	[4]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ecopipam	DMS9R43	Cocaine addiction	6C45.2	Phase 3	[5]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[6]
DAS-431	DMM3BPL	Dementia	6D80-6D86	Phase 2	[7]
Dihydrexidine	DMACPQO	Psychotic disorder	6A20-6A25	Phase 1/2	[8]
Lu AF28996	DMY572G	Parkinson disease	8A00.0	Phase 1	[9]

19 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ADROGOLIDE HYDROCHLORIDE	DMS8JIU	Cognitive impairment	6D71	Discontinued in Phase 2	[7]
ADX-10061	DMZS2M4	Psychotic disorder	6A20-6A25	Discontinued in Phase 2	[10]
BAM-1110	DMPMKUF	Parkinson disease	8A00.0	Discontinued in Phase 2	[11]
CY-208243	DMP8TKA	Pain	MG30-MG3Z	Discontinued in Phase 2	[12]
ZELANDOPAM HYDROCHLORIDE	DM1QXPE	Hypertension	BA00-BA04	Discontinued in Phase 2	[13]
Berupipam	DMU1YON	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[14]
BTS-73947	DMGVEJ6	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[15]
Odapipam	DMZN6F3	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[16]
SDZ-GLC-756	DM1C0K4	Glaucoma/ocular hypertension	9C61	Discontinued in Phase 1	[17]
A 77636	DM0NY6K	Parkinson disease	8A00.0	Terminated	[19]
A-68930	DMUJ94B	Hypertension	BA00-BA04	Terminated	[20]
A-69024	DMPL1OV	Psychotic disorder	6A20-6A25	Terminated	[21]
BIMG80	DM9X1DZ	Psychotic disorder	6A20-6A25	Terminated	[22]
CEE-03-320	DMGEFX7	Substance use disorder	6C4Z	Terminated	[23]
NNC-22-0031	DMK7BV9	Psychotic disorder	6A20-6A25	Terminated	[24]
Org-10490	DMUGC2X	Psychotic disorder	6A20-6A25	Terminated	[3]
SDZ-PSD-958	DM48MCL	Psychiatric disorder	6E8Z	Terminated	[25]
SKF 38393	DMIMJ8Z	Type-2 diabetes	5A11	Terminated	[26]
SKF-81297	DM4LGPT	Parkinson disease	8A00.0	Terminated	[27]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BSF-78438	DMO15TX	Schizophrenia	6A20	Preclinical	[18]

84 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-(1R,1'S)-berbamunine hydrochloride	DMF62GN	Discovery agent	N.A.	Investigative	[28]
(+)-(1R,1'S)-thaligrisine hydrochloride	DM521S4	Discovery agent	N.A.	Investigative	[28]
(+)-ADTN	DMXWCVY	Discovery agent	N.A.	Investigative	[29]
(+)-BUTACLAMOL	DMX6UYN	Discovery agent	N.A.	Investigative	[30]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[31]
(-)-(1S,1'R)-O,O-dimethylgrisbine hydrochloride	DM974LP	Discovery agent	N.A.	Investigative	[28]
(R)-(+)-coclaurine	DM7C148	Discovery agent	N.A.	Investigative	[32]
(R)-(-)-10-methyl-11-hydroxyaporphine	DMYJAM5	Discovery agent	N.A.	Investigative	[33]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine	DMKB621	Discovery agent	N.A.	Investigative	[34]
(R)-(-)-2-methoxy-11-hydroxyaporphine	DMQ2INJ	Discovery agent	N.A.	Investigative	[34]
(R)-(-)-2-methoxy-N-npropylnorapomorphine	DMLXB62	Discovery agent	N.A.	Investigative	[34]
(R)-(-)-N-ethyl-2-methoxy-11-hydroxynoraporphine	DMPSEZV	Discovery agent	N.A.	Investigative	[34]
(R)-(-)-N-propyl-2-methoxy-11-hydroxynoraporphine	DM48SML	Discovery agent	N.A.	Investigative	[34]
(R)-11-Amino-2-methoxyaporphine	DMKJWMC	Discovery agent	N.A.	Investigative	[35]
(R)-2,11-Diaminoaporphine	DM70ZIF	Discovery agent	N.A.	Investigative	[35]
(R,S)-homoaromaline hydrochloride	DMUG451	Discovery agent	N.A.	Investigative	[28]
(S)-BULBOCAPNINE	DMPI0AX	Discovery agent	N.A.	Investigative	[36]
(S)APOMORPHINE	DMEKGIX	Discovery agent	N.A.	Investigative	[37]
(S,S)-oxandrine hydrochloride	DMYDS6F	Discovery agent	N.A.	Investigative	[28]
1,2,3,7,12,12a-hexahydro-1-aza-pleiaden-5-ol	DMYDGAZ	Discovery agent	N.A.	Investigative	[36]
1,2,3,7,12,12a-hexahydro-1-aza-pleiadene-5,6-diol	DMAJ0B4	Discovery agent	N.A.	Investigative	[36]
1,2-Bis-[R-(-)-apomorphine-2'-oxy]ethane	DM9ENXO	Discovery agent	N.A.	Investigative	[38]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine	DMUDVRM	Discovery agent	N.A.	Investigative	[39]
1-Aminomethyl-3-cyclohexyl-isochroman-5,6-diol	DMBWNL6	Discovery agent	N.A.	Investigative	[40]
1-Aminomethyl-3-phenyl-isochroman-5,6-diol	DMJNG8A	Discovery agent	N.A.	Investigative	[41]
1-Aminomethyl-isochroman-5,6-diol	DM50GS7	Discovery agent	N.A.	Investigative	[41]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine	DMF0GXD	Discovery agent	N.A.	Investigative	[42]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine	DMBRJ5S	Discovery agent	N.A.	Investigative	[42]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine	DMSBNY8	Discovery agent	N.A.	Investigative	[42]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine	DMOL2Y0	Discovery agent	N.A.	Investigative	[43]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine	DMTNRG7	Discovery agent	N.A.	Investigative	[4]
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine	DMLSU30	Discovery agent	N.A.	Investigative	[4]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine	DMD2NXL	Discovery agent	N.A.	Investigative	[4]
11-Butyryloxy-N-n-propylnoraporphine	DMH5QEA	Discovery agent	N.A.	Investigative	[44]
11-Heptanoyloxy-N-n-propylnoraporphine	DMX4I9D	Discovery agent	N.A.	Investigative	[44]
11-Hexanoyloxy-N-n-propylnoraporphine	DMRYV9E	Discovery agent	N.A.	Investigative	[44]
11-Propionyloxy-N-n-propylnoraporphine	DM62FEH	Discovery agent	N.A.	Investigative	[44]
11-valeryloxynoraporphine	DMM91WE	Discovery agent	N.A.	Investigative	[44]
2-methoxyapomorphine	DMPG0V7	Discovery agent	N.A.	Investigative	[38]
2-Methyl-8-phenyl-1,2,3,4-tetrahydro-isoquinoline	DMY65CX	Discovery agent	N.A.	Investigative	[45]
2-{[R-(-)-Apomorphine-2'-oxy]ethoxy}-ethanol	DM9TCWA	Discovery agent	N.A.	Investigative	[38]
3,8-dibromoboldine	DM23CEI	Discovery agent	N.A.	Investigative	[46]
3-bromoboldine	DMPF7O2	Discovery agent	N.A.	Investigative	[46]
3-Chloroboldine	DM5J1TX	Discovery agent	N.A.	Investigative	[46]
3-Iodoboldine	DM890WJ	Discovery agent	N.A.	Investigative	[46]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[47]
4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine	DM08CG7	Discovery agent	N.A.	Investigative	[4]
5-(2-Amino-ethyl)-2-chloro-phenol hydrobromide	DMJXI65	Discovery agent	N.A.	Investigative	[48]
6-(2-Amino-ethyl)-biphenyl-2,3,4'-triol	DMO724D	Discovery agent	N.A.	Investigative	[49]
6-(2-Amino-ethyl)-biphenyl-2,3-diol	DMI8KOF	Discovery agent	N.A.	Investigative	[49]
6-(2-Dipropylamino-ethyl)-biphenyl-2,3,4'-triol	DM3VME7	Discovery agent	N.A.	Investigative	[49]
6-(2-Dipropylamino-ethyl)-biphenyl-2,3-diol	DMNQWZO	Discovery agent	N.A.	Investigative	[49]
9-Aminomethyl-9H-fluorene-2,5,6-triol	DM9123M	Discovery agent	N.A.	Investigative	[49]
9-Aminomethyl-9H-fluorene-3,4-diol	DMNG6O7	Discovery agent	N.A.	Investigative	[49]
BOLDINE	DMMVB5P	Discovery agent	N.A.	Investigative	[46]
Etoloxamine	DMDOX1Z	Discovery agent	N.A.	Investigative	[4]
FALCARINDIOL	DMLOV18	Discovery agent	N.A.	Investigative	[50]
FLUMEZAPINE	DMW0HOG	Discovery agent	N.A.	Investigative	[51]
FLUTROLINE	DMUOHVL	Discovery agent	N.A.	Investigative	[52]
GLAUCINE	DMSP7V8	Discovery agent	N.A.	Investigative	[36]
IBZM	DMUSRJ8	Discovery agent	N.A.	Investigative	[53]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[54]
ISOLOXAPINE	DMH1BN4	Discovery agent	N.A.	Investigative	[55]
MCL-516	DMQA7ZI	Discovery agent	N.A.	Investigative	[56]
MELOSMINE	DM3492O	Discovery agent	N.A.	Investigative	[36]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide	DMU1ATH	Discovery agent	N.A.	Investigative	[57]
N-(4-Propylaminobutyl)-4-biphenylcarboxamide	DMG9D7A	Discovery agent	N.A.	Investigative	[57]
N-propylnorapomorphine	DMO7MTX	N. A.	N. A.	Investigative	[29]
NORSTEPHALAGINE	DM1VIHC	Discovery agent	N.A.	Investigative	[36]
PUKATEINE	DM4SGVF	Discovery agent	N.A.	Investigative	[36]
QUINPIROLE	DMDNHEP	Discovery agent	N.A.	Investigative	[58]
Ro-21-7767	DMOE0JX	Discovery agent	N.A.	Investigative	[59]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[60]
SCH-12679	DMP8OKA	Discovery agent	N.A.	Investigative	[61]
SCH-23390	DMT1OAH	N. A.	N. A.	Investigative	[62]
SCH-24518	DM6SC5K	Discovery agent	N.A.	Investigative	[63]
SK&F-89626	DM3SUKX	Discovery agent	N.A.	Investigative	[64]
SKF-75670	DMQ6YXF	Discovery agent	N.A.	Investigative	[65]
SKF-83556	DMCMQH8	Discovery agent	N.A.	Investigative	[29]
SKF-83959	DMWC6RU	Discovery agent	N.A.	Investigative	[66]
STEPHOLIDINE	DMGMXQC	Discovery agent	N.A.	Investigative	[67]
TEPA (possesses cytotoxic activity)	DMROS5K	Discovery agent	N.A.	Investigative	[68]
[125I]SCH23982	DM06S9X	Discovery agent	N.A.	Investigative	[69]
[R-(-)-Apomorphine-2-yl]-(2'-hydroxy-ethyl)ether	DM8YF3V	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
Schizophrenia	6A20	Pre-frontal cortex	2.79E-02	-0.53	-0.53
Schizophrenia	6A20	Superior temporal cortex	4.77E-01	0.1	0.26
Parkinson's disease	8A00.0	Substantia nigra tissue	8.99E-01	-0.06	-0.3
Type 2 diabetes	5A11	Liver tissue	3.08E-01	-0.02	-0.14

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