Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4C8EA)

• DTT Name: Dopamine D3 receptor (D3R)
• Synonyms: D(3) dopamine receptor
• Gene Name: DRD3
• DTT Type: Successful target; [1]
• Related Disease:
  Bipolar disorder [ICD-11: 6A60]
  Parkinsonism [ICD-11: 8A00]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: DRD3_HUMAN
• TTD ID: T02551
• Sequence:
  MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
  QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN
  LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV
  CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ
  QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK
  LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV
  SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC
• Function: Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Dopamine receptors (R-HSA-390651)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cariprazine	DMJYDVK	Bipolar disorder	6A60	Approved	[1]
Pramipexole	DMNMW9R	Parkinson disease	8A00.0	Approved	[2]
Ropinirole	DMA6S1D	Parkinson disease	8A00.0	Approved	[2]

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[3]
P2B-001	DM9PVHX	Parkinson disease	8A00.0	Phase 3	[4]
GSK598809	DMGU05N	Drug abuse	6C4G.1Z	Phase 2	[5]
ONC201	DMM5SCF	Endometrial cancer	2C76	Phase 2	[6]
RP5063	DMKUE8O	Schizophrenia	6A20	Phase 2	[7]
TAK-906	DMBQD9H	Diabetic gastroparesis	DA41.00	Phase 2	[8]
GSK618334	DMJPXZ4	Drug abuse	6C4G.1Z	Phase 1	[5]
Pfizer 10	DM6ER9L	Female sexual arousal dysfunction	HA01.1	Phase 1	[9]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aryl piperazine derivative 1	DM9DJGU	N. A.	N. A.	Patented	[10]
Aryl piperazine derivative 6	DMZ3DS5	N. A.	N. A.	Patented	[10]

17 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quinelorane	DMO9XTJ	Male sexual disorder	HA02.0	Discontinued in Phase 3	[11]
A-437203	DMEG240	Psychotic disorder	6A20-6A25	Discontinued in Phase 2	[12]
BP-897	DMAQ6DS	Cocaine addiction	6C45.2	Discontinued in Phase 2	[13]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[14]
AVE-5997EF	DM5FDX2	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[15]
S-33138	DM1R8Z7	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[16], [17]
AS-8112	DMIFDPL	Vomiting	MD90	Terminated	[21]
BP4.879a	DMN8FAG	Schizophrenia	6A20	Terminated	[15]
BTS-79018	DMAH3Z9	Schizophrenia	6A20	Terminated	[15]
Dianicline+rimonabant	DM6LP0R	Tobacco dependence	6C4A.2	Terminated	[22]
E-2040	DMZWU8V	Schizophrenia	6A20	Terminated	[23]
GR-218231	DMIJCH1	N. A.	N. A.	Terminated	[24]
PNU-177864	DMRT69H	Schizophrenia	6A20	Terminated	[15]
PNU-96391A	DMLMISK	Substance use disorder	6C4Z	Terminated	[25]
RGH-1756	DM8RIA6	Schizophrenia	6A20	Terminated	[15]
SB-277011	DM3M16Q	Schizophrenia	6A20	Terminated	[15]
YM-43611	DMWI094	Psychotic disorder	6A20-6A25	Terminated	[26]

7 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
F-15063	DMUFP05	Schizophrenia	6A20	Preclinical	[18]
PD-157533	DMTG730	Schizophrenia	6A20	Preclinical	[15]
PD-157695	DMDSR1X	Schizophrenia	6A20	Preclinical	[15]
PD-158771	DM682UV	Schizophrenia	6A20	Preclinical	[15]
S-33084	DMWQ3TH	Psychotic disorder	6A20-6A25	Preclinical	[19]
S32504	DM4V8ZD	Parkinson disease	8A00.0	Preclinical	[20]
U-99194A	DMW87JR	Schizophrenia	6A20	Preclinical	[15]

86 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-AJ76	DMEDMC0	Discovery agent	N.A.	Investigative	[27]
(+)-BUTACLAMOL	DMX6UYN	Discovery agent	N.A.	Investigative	[28]
(+)-S-14297	DMX7ECD	Discovery agent	N.A.	Investigative	[29]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[30]
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile	DME5TIR	Discovery agent	N.A.	Investigative	[31]
(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine	DMFRPGX	Discovery agent	N.A.	Investigative	[32]
(4-Dipropylamino-cyclohexylidene)-acetonitrile	DMRIWH2	Discovery agent	N.A.	Investigative	[33]
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine	DMHQCRU	Discovery agent	N.A.	Investigative	[34]
(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine	DMQM8O5	Discovery agent	N.A.	Investigative	[33]
(R)-(-)-2-Methyl-apomorphine hydrochloride	DMAYEJL	Discovery agent	N.A.	Investigative	[35]
(R)-(-)-2-Phenyl-apomorphine hydrochloride	DME62U0	Discovery agent	N.A.	Investigative	[35]
(R)-2-(Benzylamino-methyl)-chroman-7-ol	DMJVQN8	Discovery agent	N.A.	Investigative	[36]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine	DMUDVRM	Discovery agent	N.A.	Investigative	[37]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one	DMM18AQ	Discovery agent	N.A.	Investigative	[38]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine	DMF0GXD	Discovery agent	N.A.	Investigative	[39]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine	DMBRJ5S	Discovery agent	N.A.	Investigative	[39]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine	DMSBNY8	Discovery agent	N.A.	Investigative	[39]
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine	DMCJZVA	Discovery agent	N.A.	Investigative	[39]
1-Benzyl-4-pyrrol-1-yl-piperidine	DMNWEC9	Discovery agent	N.A.	Investigative	[39]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine	DMOL2Y0	Discovery agent	N.A.	Investigative	[40]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine	DMOCAUL	Discovery agent	N.A.	Investigative	[41]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine	DMTNRG7	Discovery agent	N.A.	Investigative	[32]
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine	DMLSU30	Discovery agent	N.A.	Investigative	[32]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine	DMD2NXL	Discovery agent	N.A.	Investigative	[32]
2-(4-Dipropylamino-cyclohexylidene)-malononitrile	DMXH0FO	Discovery agent	N.A.	Investigative	[33]
3-(1-Propyl-pyrrolidin-3-yl)-phenol	DM4QRV9	Discovery agent	N.A.	Investigative	[41]
3-(2-Benzylamino-ethoxy)-phenol	DMZCTGF	Discovery agent	N.A.	Investigative	[42]
3-(4-Benzyl-piperazin-1-yl)-phenol	DMWPB0G	Discovery agent	N.A.	Investigative	[43]
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole	DM0HYDZ	Discovery agent	N.A.	Investigative	[44]
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole	DM17SNR	Discovery agent	N.A.	Investigative	[44]
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole	DMM0WGI	Discovery agent	N.A.	Investigative	[44]
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one	DMYVD2E	Discovery agent	N.A.	Investigative	[42]
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole	DMXAEW9	Discovery agent	N.A.	Investigative	[43]
4-(4-Benzyl-piperazin-1-yl)-1H-indole	DMWR0AS	Discovery agent	N.A.	Investigative	[43]
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole	DMZ4237	Discovery agent	N.A.	Investigative	[43]
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole	DMVAB7U	Discovery agent	N.A.	Investigative	[43]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[45]
4-Dipropylamino-cyclohex-1-enecarbonitrile	DMKEHLD	Discovery agent	N.A.	Investigative	[33]
5-OH-DPAT	DMZT6JR	Discovery agent	N.A.	Investigative	[46]
7-trans-OH-PIPAT	DMOQMA0	Discovery agent	N.A.	Investigative	[47]
A-690344	DMT6A7G	Schizophrenia	6A20	Investigative	[48]
A-706149	DMXOPFU	Discovery agent	N.A.	Investigative	[49]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[28]
AS-9705	DMR01O4	Gastric motility disorder	DA21	Investigative	[21]
Azaperone	DMKI2GJ	Discovery agent	N.A.	Investigative	[50]
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine	DMTC4G0	Discovery agent	N.A.	Investigative	[42]
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine	DMV6DY7	Discovery agent	N.A.	Investigative	[42]
D-189	DMU8BJH	Discovery agent	N.A.	Investigative	[51]
D-190	DMUMNSW	Discovery agent	N.A.	Investigative	[51]
D-192	DM8D26T	Discovery agent	N.A.	Investigative	[51]
D-193	DMU83T7	Discovery agent	N.A.	Investigative	[51]
D-203	DMKPIH0	Discovery agent	N.A.	Investigative	[51]
D-210	DMNLE4S	Discovery agent	N.A.	Investigative	[51]
D-218	DMQLT84	Discovery agent	N.A.	Investigative	[51]
D-219	DMQ2U4G	Discovery agent	N.A.	Investigative	[51]
D-220	DMTUJWN	Discovery agent	N.A.	Investigative	[51]
D-237	DMGA48T	Discovery agent	N.A.	Investigative	[52]
D-264	DMWLHBQ	Discovery agent	N.A.	Investigative	[53]
D-315	DMG1CD5	Discovery agent	N.A.	Investigative	[54]
D-366	DMZAM3G	Discovery agent	N.A.	Investigative	[46]
Etoloxamine	DMDOX1Z	Discovery agent	N.A.	Investigative	[32]
FLUMEZAPINE	DMW0HOG	Discovery agent	N.A.	Investigative	[55]
FLUTROLINE	DMUOHVL	Discovery agent	N.A.	Investigative	[56]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[40]
ISOLOXAPINE	DMH1BN4	Discovery agent	N.A.	Investigative	[57]
L-741626	DMCYQJF	Discovery agent	N.A.	Investigative	[58]
L-741742	DMP75YK	Discovery agent	N.A.	Investigative	[59]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide	DMU1ATH	Discovery agent	N.A.	Investigative	[34]
N-(4-Propylaminobutyl)-4-biphenylcarboxamide	DMG9D7A	Discovery agent	N.A.	Investigative	[34]
N-propylnorapomorphine	DMO7MTX	N. A.	N. A.	Investigative	[60]
nafadotride	DM79KLR	Discovery agent	N.A.	Investigative	[61]
NGB 2904	DMMC42Z	Discovery agent	N.A.	Investigative	[62]
PD 128907	DMYC51H	Discovery agent	N.A.	Investigative	[63], [64]
PD-152255	DMV0EDM	Discovery agent	N.A.	Investigative	[65]
PF-592379	DMY93GJ	Discovery agent	N.A.	Investigative	[66]
PG-01037	DM2TP4Q	Discovery agent	N.A.	Investigative	[67]
piribedil	DMNP6QD	Discovery agent	N.A.	Investigative	[68]
QUINPIROLE	DMDNHEP	Discovery agent	N.A.	Investigative	[69]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[70]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[71]
SB269652	DMEGNJK	Discovery agent	N.A.	Investigative	[72]
STEPHOLIDINE	DMGMXQC	Discovery agent	N.A.	Investigative	[73]
UH-232	DM5K6ZE	Discovery agent	N.A.	Investigative	[74]
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine	DMSPMHE	Discovery agent	N.A.	Investigative	[42]
[3H]7-OH-DPAT	DM2PW8T	Discovery agent	N.A.	Investigative	[75], [52], [76]
[3H]spiperone	DMWHEV8	Discovery agent	N.A.	Investigative	[77], [78]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Parkinson's disease	8A00.0	Substantia nigra tissue	2.84E-03	0.13	2
Bipolar disorder	6A20	Pre-frontal cortex	1.88E-01	-0.03	-0.25
Schizophrenia	6A20	Pre-frontal cortex	5.74E-02	0.05	0.34
Schizophrenia	6A20	Superior temporal cortex	2.15E-01	-0.05	-0.46

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