Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T02551
(Former ID: TTDS00013)
|
|||||
| Target Name |
Dopamine D3 receptor (D3R)
|
|||||
| Synonyms |
D(3) dopamine receptor
Click to Show/Hide
|
|||||
| Gene Name |
DRD3
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Bipolar disorder [ICD-11: 6A60] | |||||
| 2 | Parkinsonism [ICD-11: 8A00] | |||||
| Function |
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Click to Show/Hide
|
|||||
| BioChemical Class |
GPCR rhodopsin
|
|||||
| UniProt ID | ||||||
| Sequence |
MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A04234 | |||||
| HIT2.0 ID | T43Y5O | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
| 1 | Cariprazine | Drug Info | Approved | Bipolar disorder | [1], [2] | |
| 2 | Pramipexole | Drug Info | Approved | Parkinson disease | [3], [4] | |
| 3 | Ropinirole | Drug Info | Approved | Parkinson disease | [5], [6] | |
| Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
| 1 | CM-2395 | Drug Info | Phase 3 | Schizophrenia | [7] | |
| 2 | P2B-001 | Drug Info | Phase 3 | Parkinson disease | [8] | |
| 3 | GSK598809 | Drug Info | Phase 2 | Drug abuse | [9] | |
| 4 | ONC201 | Drug Info | Phase 2 | Glioma | [8], [10] | |
| 5 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [11] | |
| 6 | TAK-906 | Drug Info | Phase 2 | Diabetic gastroparesis | [12] | |
| 7 | GSK618334 | Drug Info | Phase 1 | Drug abuse | [13] | |
| 8 | Pfizer 10 | Drug Info | Phase 1 | Female sexual arousal dysfunction | [14] | |
| Discontinued Drug(s) | [+] 15 Discontinued Drugs | + | ||||
| 1 | Quinelorane | Drug Info | Discontinued in Phase 3 | Male sexual disorder | [15], [16] | |
| 2 | A-437203 | Drug Info | Discontinued in Phase 2 | Psychotic disorder | [17] | |
| 3 | BP-897 | Drug Info | Discontinued in Phase 2 | Cocaine addiction | [18], [19] | |
| 4 | AVE-5997EF | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [20] | |
| 5 | S-33138 | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [21] | |
| 6 | AS-8112 | Drug Info | Terminated | Vomiting | [27] | |
| 7 | BP4.879a | Drug Info | Terminated | Schizophrenia | [23] | |
| 8 | BTS-79018 | Drug Info | Terminated | Schizophrenia | [23] | |
| 9 | Dianicline+rimonabant | Drug Info | Terminated | Tobacco dependence | [28] | |
| 10 | E-2040 | Drug Info | Terminated | Schizophrenia | [29] | |
| 11 | PNU-177864 | Drug Info | Terminated | Schizophrenia | [23] | |
| 12 | PNU-96391A | Drug Info | Terminated | Substance use disorder | [30] | |
| 13 | RGH-1756 | Drug Info | Terminated | Schizophrenia | [23] | |
| 14 | SB-277011 | Drug Info | Terminated | Schizophrenia | [23], [31] | |
| 15 | YM-43611 | Drug Info | Terminated | Psychotic disorder | [32] | |
| Preclinical Drug(s) | [+] 7 Preclinical Drugs | + | ||||
| 1 | F-15063 | Drug Info | Preclinical | Schizophrenia | [22] | |
| 2 | PD-157533 | Drug Info | Preclinical | Schizophrenia | [23] | |
| 3 | PD-157695 | Drug Info | Preclinical | Schizophrenia | [23] | |
| 4 | PD-158771 | Drug Info | Preclinical | Schizophrenia | [23] | |
| 5 | S-33084 | Drug Info | Preclinical | Psychotic disorder | [24], [25] | |
| 6 | S32504 | Drug Info | Preclinical | Parkinson disease | [26] | |
| 7 | U-99194A | Drug Info | Preclinical | Schizophrenia | [23] | |
| Mode of Action | [+] 8 Modes of Action | + | ||||
| Modulator | [+] 13 Modulator drugs | + | ||||
| 1 | Cariprazine | Drug Info | [1] | |||
| 2 | Pramipexole | Drug Info | [33] | |||
| 3 | Ropinirole | Drug Info | [33] | |||
| 4 | Quinelorane | Drug Info | [40] | |||
| 5 | A-437203 | Drug Info | [41] | |||
| 6 | BP-897 | Drug Info | [42] | |||
| 7 | F-15063 | Drug Info | [46] | |||
| 8 | S-33084 | Drug Info | [47] | |||
| 9 | S32504 | Drug Info | [26] | |||
| 10 | E-2040 | Drug Info | [50] | |||
| 11 | PNU-96391A | Drug Info | [30] | |||
| 12 | YM-43611 | Drug Info | [52] | |||
| 13 | PD-152255 | Drug Info | [91] | |||
| Agonist | [+] 8 Agonist drugs | + | ||||
| 1 | CM-2395 | Drug Info | [34] | |||
| 2 | Pfizer 10 | Drug Info | [14] | |||
| 3 | 7-trans-OH-PIPAT | Drug Info | [73] | |||
| 4 | N-propylnorapomorphine | Drug Info | [86] | |||
| 5 | PD 128907 | Drug Info | [89], [90] | |||
| 6 | PF-592379 | Drug Info | [92] | |||
| 7 | piribedil | Drug Info | [94] | |||
| 8 | [3H]7-OH-DPAT | Drug Info | [78], [101], [102] | |||
| Inhibitor | [+] 76 Inhibitor drugs | + | ||||
| 1 | P2B-001 | Drug Info | [35] | |||
| 2 | TAK-906 | Drug Info | [38] | |||
| 3 | MAZAPERTINE | Drug Info | [43] | |||
| 4 | GR-218231 | Drug Info | [51] | |||
| 5 | (+)-BUTACLAMOL | Drug Info | [54] | |||
| 6 | (+/-)-nantenine | Drug Info | [56] | |||
| 7 | (-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile | Drug Info | [57] | |||
| 8 | (2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine | Drug Info | [58] | |||
| 9 | (4-Dipropylamino-cyclohexylidene)-acetonitrile | Drug Info | [59] | |||
| 10 | (4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine | Drug Info | [60] | |||
| 11 | (4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine | Drug Info | [59] | |||
| 12 | (R)-(-)-2-Methyl-apomorphine hydrochloride | Drug Info | [61] | |||
| 13 | (R)-(-)-2-Phenyl-apomorphine hydrochloride | Drug Info | [61] | |||
| 14 | (R)-2-(Benzylamino-methyl)-chroman-7-ol | Drug Info | [62] | |||
| 15 | 1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine | Drug Info | [63] | |||
| 16 | 1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one | Drug Info | [64] | |||
| 17 | 1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine | Drug Info | [65] | |||
| 18 | 1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine | Drug Info | [65] | |||
| 19 | 1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine | Drug Info | [65] | |||
| 20 | 1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine | Drug Info | [65] | |||
| 21 | 1-Benzyl-4-pyrrol-1-yl-piperidine | Drug Info | [65] | |||
| 22 | 1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine | Drug Info | [66] | |||
| 23 | 1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [67] | |||
| 24 | 1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine | Drug Info | [58] | |||
| 25 | 1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine | Drug Info | [58] | |||
| 26 | 1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine | Drug Info | [58] | |||
| 27 | 2-(4-Dipropylamino-cyclohexylidene)-malononitrile | Drug Info | [59] | |||
| 28 | 3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | [67] | |||
| 29 | 3-(2-Benzylamino-ethoxy)-phenol | Drug Info | [68] | |||
| 30 | 3-(4-Benzyl-piperazin-1-yl)-phenol | Drug Info | [69] | |||
| 31 | 3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole | Drug Info | [70] | |||
| 32 | 3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole | Drug Info | [70] | |||
| 33 | 3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole | Drug Info | [70] | |||
| 34 | 4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one | Drug Info | [68] | |||
| 35 | 4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole | Drug Info | [69] | |||
| 36 | 4-(4-Benzyl-piperazin-1-yl)-1H-indole | Drug Info | [69] | |||
| 37 | 4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole | Drug Info | [69] | |||
| 38 | 4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole | Drug Info | [69] | |||
| 39 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [71] | |||
| 40 | 4-Dipropylamino-cyclohex-1-enecarbonitrile | Drug Info | [59] | |||
| 41 | 5-OH-DPAT | Drug Info | [72] | |||
| 42 | A-690344 | Drug Info | [74] | |||
| 43 | A-706149 | Drug Info | [75] | |||
| 44 | A-987306 | Drug Info | [54] | |||
| 45 | Azaperone | Drug Info | [76] | |||
| 46 | Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine | Drug Info | [68] | |||
| 47 | Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine | Drug Info | [68] | |||
| 48 | D-189 | Drug Info | [77] | |||
| 49 | D-190 | Drug Info | [77] | |||
| 50 | D-192 | Drug Info | [77] | |||
| 51 | D-193 | Drug Info | [77] | |||
| 52 | D-203 | Drug Info | [77] | |||
| 53 | D-210 | Drug Info | [77] | |||
| 54 | D-218 | Drug Info | [77] | |||
| 55 | D-219 | Drug Info | [77] | |||
| 56 | D-220 | Drug Info | [77] | |||
| 57 | D-237 | Drug Info | [78] | |||
| 58 | D-264 | Drug Info | [79] | |||
| 59 | D-315 | Drug Info | [80] | |||
| 60 | D-366 | Drug Info | [72] | |||
| 61 | Etoloxamine | Drug Info | [58] | |||
| 62 | FLUMEZAPINE | Drug Info | [81] | |||
| 63 | FLUTROLINE | Drug Info | [82] | |||
| 64 | ISOCLOZAPINE | Drug Info | [66] | |||
| 65 | ISOLOXAPINE | Drug Info | [83] | |||
| 66 | L-741626 | Drug Info | [84] | |||
| 67 | L-741742 | Drug Info | [85] | |||
| 68 | N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide | Drug Info | [60] | |||
| 69 | N-(4-Propylaminobutyl)-4-biphenylcarboxamide | Drug Info | [60] | |||
| 70 | PG-01037 | Drug Info | [93] | |||
| 71 | QUINPIROLE | Drug Info | [95] | |||
| 72 | R-226161 | Drug Info | [96] | |||
| 73 | SB-271046 | Drug Info | [97] | |||
| 74 | STEPHOLIDINE | Drug Info | [99] | |||
| 75 | UH-232 | Drug Info | [100] | |||
| 76 | [2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine | Drug Info | [68] | |||
| Antagonist | [+] 20 Antagonist drugs | + | ||||
| 1 | GSK598809 | Drug Info | [36] | |||
| 2 | ONC201 | Drug Info | [10] | |||
| 3 | GSK618334 | Drug Info | [36] | |||
| 4 | AVE-5997EF | Drug Info | [23] | |||
| 5 | S-33138 | Drug Info | [44], [45] | |||
| 6 | PD-157533 | Drug Info | [23] | |||
| 7 | PD-157695 | Drug Info | [23] | |||
| 8 | PD-158771 | Drug Info | [23] | |||
| 9 | AS-8112 | Drug Info | [48] | |||
| 10 | BP4.879a | Drug Info | [23] | |||
| 11 | Dianicline+rimonabant | Drug Info | [49] | |||
| 12 | PNU-177864 | Drug Info | [23] | |||
| 13 | RGH-1756 | Drug Info | [23] | |||
| 14 | SB-277011 | Drug Info | [23] | |||
| 15 | (+)-AJ76 | Drug Info | [53] | |||
| 16 | (+)-S-14297 | Drug Info | [55] | |||
| 17 | AS-9705 | Drug Info | [48] | |||
| 18 | nafadotride | Drug Info | [87] | |||
| 19 | NGB 2904 | Drug Info | [88] | |||
| 20 | [3H]spiperone | Drug Info | [103], [104] | |||
| Partial agonist | [+] 1 Partial agonist drugs | + | ||||
| 1 | RP5063 | Drug Info | [37] | |||
| Ligand | [+] 2 Ligand drugs | + | ||||
| 1 | Aryl piperazine derivative 1 | Drug Info | [39] | |||
| 2 | Aryl piperazine derivative 6 | Drug Info | [39] | |||
| Binder | [+] 2 Binder drugs | + | ||||
| 1 | U-99194A | Drug Info | [23] | |||
| 2 | BTS-79018 | Drug Info | [23] | |||
| Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
| 1 | SB269652 | Drug Info | [98] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Eticlopride | Ligand Info | |||||
| Structure Description | Structure of the human dopamine D3 receptor in complex with eticlopride | PDB:3PBL | ||||
| Method | X-ray diffraction | Resolution | 2.89 Å | Mutation | Yes | [105] |
| PDB Sequence |
YALSYCALIL
41 AIVFGNGLVC51 MAVLKERALQ61 TTTNYLVVSL71 AVADLLVATL81 VMPWVVYLEV 91 TGGVWNFSRI101 CCDVFVTLDV111 MMCTASIWNL121 CAISIDRYTA131 VVMPVHYQHG 141 TGQSSCRRVA151 LMITAVWVLA161 FAVSCPLLFG171 FNTTGDPTVC181 SISNPDFVIY 191 SSVVSFYLPF201 GVTVLVYARI211 YVVLKQRRRK221 NIFEMLRIDE1011 GLRLKIYKDT 1021 EGYYTIGIGH1031 LLTKSPSLNA1041 AKSELDKAIG1051 RNTNGVITKD1061 EAEKLFNQDV 1071 DAAVRGILRN1081 AKLKPVYDSL1091 DAVRRAALIN1101 MVFQMGETGV1111 AGFTNSLRML 1121 QQKRWDEAAV1131 NLAKSRWYNQ1141 TPNRAKRVIT1151 TFRTGTWDAY1161 GVPLREKKAT 328 QMVAIVLGAF338 IVCWLPFFLT348 HVLNTHCQTC358 HVSPELYSAT368 TWLGYVNSAL 378 NPVIYTTFNI388 EFRKAFLKIL398 SC
|
|||||
|
|
VAL86
4.444
PHE106
3.635
VAL107
4.269
ASP110
2.702
VAL111
3.444
CYS114
3.583
THR115
4.791
ILE183
3.496
VAL189
3.756
SER192
3.330
|
|||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
|
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Dopaminergic synapse | hsa04728 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| 2 | Dopaminergic synapse | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Dopamine receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 6 WikiPathways | + | ||||
| 1 | Monoamine GPCRs | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| 5 | Nicotine Activity on Dopaminergic Neurons | |||||
| 6 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7671). | |||||
| REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 953). | |||||
| REF 4 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7295). | |||||
| REF 6 | Update on ropinirole in the treatment of Parkinson's disease. Neuropsychiatr Dis Treat. 2009;5:33-6. | |||||
| REF 7 | Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010. | |||||
| REF 8 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 9 | ClinicalTrials.gov (NCT01188967) Effectiveness of GSK598809, a Selective D3 Antagonist, Added to Cognitive Behavioral Therapy and Nicotine Replacement Therapy for Smoking Cessation and Prevention of Very Early Relapse to Smoking. U.S. National Institutes of Health. | |||||
| REF 10 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 11 | ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health. | |||||
| REF 12 | ClinicalTrials.gov (NCT03544229) A Study to Evaluate the Efficacy and Safety of TAK-906 in Adult Participants With Symptomatic Idiopathic or Diabetic Gastroparesis. U.S. National Institutes of Health. | |||||
| REF 13 | ClinicalTrials.gov (NCT00513279) To Investigate If Single Doses Of GSK618334 Are Safe And To Investigate Blood Levels Of GSK618334. U.S. National Institutes of Health. | |||||
| REF 14 | Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. | |||||
| REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 954). | |||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001472) | |||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012940) | |||||
| REF 18 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7625). | |||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012397) | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018413) | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014544) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026348) | |||||
| REF 23 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
| REF 24 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 129). | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013394) | |||||
| REF 26 | S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity ... J Pharmacol Exp Ther. 2004 Jun;309(3):921-35. | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009088) | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143) | |||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126) | |||||
| REF 30 | The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects. Neuropsychopharmacology. 2015 Jan;40(2):472-9. | |||||
| REF 31 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 143). | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005975) | |||||
| REF 33 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127) | |||||
| REF 35 | Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51. | |||||
| REF 36 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
| REF 37 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 38 | Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Jan 18. | |||||
| REF 39 | 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689. | |||||
| REF 40 | Quinelorane, a dopamine D3/D2 receptor agonist, reduces prepulse inhibition of startle and ventral pallidal GABA efflux: time course studies.Pharmacol Biochem Behav.2008 Oct;90(4):686-90. | |||||
| REF 41 | Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response.Transl Psychiatry.2013 Apr 9;3:e245. | |||||
| REF 42 | BP 897, a selective dopamine D3 receptor ligand with therapeutic potential for the treatment of cocaine-addiction.CNS Drug Rev.2003 Summer;9(2):141-58. | |||||
| REF 43 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2. | |||||
| REF 44 | The dopamine D3 receptor antagonist, S33138, counters cognitive impairment in a range of rodent and primate procedures. Int J Neuropsychopharmacol. 2010 Sep;13(8):1035-51. | |||||
| REF 45 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 46 | F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial agonist properties: (IV) duration of brain D2-like receptor occupancy and antipsychotic-like activity versus plasma concentration in mice.Naunyn Schmiedebergs Arch Pharmacol.2007 Jun;375(4):241-50. | |||||
| REF 47 | S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: II. Functional and behavioral profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther. 2000 Jun;293(3):1063-73. | |||||
| REF 48 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | |||||
| REF 49 | Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. J Neurochem. 2003 Nov;87(3):631-41. | |||||
| REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126) | |||||
| REF 51 | Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of t... Bioorg Med Chem. 2009 Jan 15;17(2):758-66. | |||||
| REF 52 | Effects of YM-43611, a novel dopamine D2-like receptor antagonist, on immediate early gene expression in the rat forebrain. Neuropsychopharmacology. 1997 Jul;17(1):27-33. | |||||
| REF 53 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990 Sep 13;347(6289):146-51. | |||||
| REF 54 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8. | |||||
| REF 55 | S 14297, a novel selective ligand at cloned human dopamine D3 receptors, blocks 7-OH-DPAT-induced hypothermia in rats. Eur J Pharmacol. 1994 Aug 1;260(2-3):R3-5. | |||||
| REF 56 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
| REF 57 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. J Med Chem. 1993 Oct 15;36(21):3188-96. | |||||
| REF 58 | Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8. | |||||
| REF 59 | Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonis... J Med Chem. 2000 Feb 24;43(4):756-62. | |||||
| REF 60 | Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. J Med Chem. 2008 Nov 13;51(21):6829-38. | |||||
| REF 61 | Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines. Bioorg Med Chem. 2008 Apr 1;16(7):3773-9. | |||||
| REF 62 | Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybri... J Med Chem. 2003 Oct 9;46(21):4377-92. | |||||
| REF 63 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2955-9. | |||||
| REF 64 | Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand. Bioorg Med Chem. 2007 Sep 1;15(17):5811-8. | |||||
| REF 65 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6. | |||||
| REF 66 | Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1982 Jul;25(7):855-8. | |||||
| REF 67 | Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997). | |||||
| REF 68 | New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8. | |||||
| REF 69 | New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80. | |||||
| REF 70 | 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4... J Med Chem. 1996 May 10;39(10):1941-2. | |||||
| REF 71 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
| REF 72 | Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a... J Med Chem. 2010 Feb 11;53(3):1023-37. | |||||
| REF 73 | Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors. J Med Chem. 1994 Nov 25;37(24):4245-50. | |||||
| REF 74 | Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives. Bioorg Med Chem Lett. 2006 Feb;16(3):490-4. | |||||
| REF 75 | Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.genes... Bioorg Med Chem Lett. 2006 Feb;16(3):658-62. | |||||
| REF 76 | Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors. J Med Chem. 1993 Nov 26;36(24):3929-36. | |||||
| REF 77 | Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly... J Med Chem. 2008 May 22;51(10):3005-19. | |||||
| REF 78 | Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding character... J Med Chem. 2008 Dec 25;51(24):7806-19. | |||||
| REF 79 | Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-... Bioorg Med Chem. 2009 Jun 1;17(11):3923-33. | |||||
| REF 80 | Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template... Bioorg Med Chem. 2010 Aug 1;18(15):5661-74. | |||||
| REF 81 | Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. J Med Chem. 1982 Oct;25(10):1133-40. | |||||
| REF 82 | Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. J Med Chem. 1980 Jun;23(6):635-43. | |||||
| REF 83 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6. | |||||
| REF 84 | Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626. Bioorg Med Chem. 2010 Jul 15;18(14):5291-300. | |||||
| REF 85 | 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. J Med Chem. 1996 May 10;39(10):1943-5. | |||||
| REF 86 | A functional test identifies dopamine agonists selective for D3 versus D2 receptors. Neuroreport. 1995 Jan 26;6(2):329-32. | |||||
| REF 87 | Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents. J Pharmacol Exp Ther. 1995 Dec;275(3):1239-46. | |||||
| REF 88 | Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction. CNS Drug Rev. 2007 Summer;13(2):240-59. | |||||
| REF 89 | Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907. J Pharmacol Exp Ther. 1995 Dec;275(3):1355-66. | |||||
| REF 90 | Characterization of binding of [3H]PD 128907, a selective dopamine D3 receptor agonist ligand, to CHO-K1 cells. Life Sci. 1995;57(15):1401-10. | |||||
| REF 91 | Pharmacological characterization of PD 152255, a novel dimeric benzimidazole dopamine D3 antagonist. Pharmacol Biochem Behav. 1998 Feb;59(2):487-93. | |||||
| REF 92 | Lack of abuse potential in a highly selective dopamine D3 agonist, PF-592,379, in drug self-administration and drug discrimination in rats. Behav Pharmacol. 2012 Jun;23(3):280-91. | |||||
| REF 93 | Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46. | |||||
| REF 94 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. | |||||
| REF 95 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. J Med Chem. 2009 Nov 12;52(21):6860-70. | |||||
| REF 96 | Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. | |||||
| REF 97 | Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. | |||||
| REF 98 | Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists. Eur Neuropsychopharmacol. 2015 Sep;25(9):1448-61. | |||||
| REF 99 | Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities Bioorg Med Chem. 2009 Oct 1;17(19):6898-907. | |||||
| REF 100 | (Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997). | |||||
| REF 101 | Radioligand binding characterization of putative dopamine D3 receptor in human peripheral blood lymphocytes with [3H]7-OH-DPAT. J Neuroimmunol. 1995 May;58(2):139-44. | |||||
| REF 102 | 7-OH-DPAT and PD 128907 selectively activate the D3 dopamine receptor in a novel environment. Neuropsychopharmacology. 2003 Jan;28(1):100-7. | |||||
| REF 103 | Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol. 2000 Jul;130(5):1045-59. | |||||
| REF 104 | Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes. J Med Chem. 2005 Feb 10;48(3):694-709. | |||||
| REF 105 | Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. Science. 2010 Nov 19;330(6007):1091-5. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.