Target Information
| Target General Information | Top | |||||
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| Target ID |
T46828
(Former ID: TTDS00015)
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| Target Name |
Dopamine D5 receptor (D5R)
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| Synonyms |
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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| Gene Name |
DRD5
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Allergic/hypersensitivity disorder [ICD-11: 4A80-4A8Z] | |||||
| Function |
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MLPPGSNGTAYPGQFALYQQLAQGNAVGGSAGAPPLGPSQVVTACLLTLLIIWTLLGNVL
VCAAIVRSRHLRANMTNVFIVSLAVSDLFVALLVMPWKAVAEVAGYWPFGAFCDVWVAFD IMCSTASILNLCVISVDRYWAISRPFRYKRKMTQRMALVMVGLAWTLSILISFIPVQLNW HRDQAASWGGLDLPNNLANWTPWEEDFWEPDVNAENCDSSLNRTYAISSSLISFYIPVAI MIVTYTRIYRIAQVQIRRISSLERAAEHAQSCRSSAACAPDTSLRASIKKETKVLKTLSV IMGVFVCCWLPFFILNCMVPFCSGHPEGPPAGFPCVSETTFDVFVWFGWANSSLNPVIYA FNADFQKVFAQLLGCSHFCSRTPVETVNISNELISYNQDIVFHKEIAAAYIHMMPNAVTP GNREVDNDEEEGPFDRMFQIYQTSPDGDPVAESVWELDCEGEISLDKITPFTPNGFH Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Phenyltoloxamine | Drug Info | Approved | Allergy | [2] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | LE-300 | Drug Info | Preclinical | Schizophrenia | [3] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | GMC-283 | Drug Info | Terminated | Schizophrenia | [3] | |
| 2 | ZD-3638 | Drug Info | Terminated | Schizophrenia | [3] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 13 Inhibitor drugs | + | ||||
| 1 | Phenyltoloxamine | Drug Info | [1] | |||
| 2 | (+/-)-nantenine | Drug Info | [5] | |||
| 3 | 1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one | Drug Info | [6] | |||
| 4 | 1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine | Drug Info | [7] | |||
| 5 | 1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine | Drug Info | [1] | |||
| 6 | 1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine | Drug Info | [1] | |||
| 7 | 1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine | Drug Info | [1] | |||
| 8 | 4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine | Drug Info | [1] | |||
| 9 | FLUMEZAPINE | Drug Info | [8] | |||
| 10 | FLUTROLINE | Drug Info | [9] | |||
| 11 | ISOCLOZAPINE | Drug Info | [7] | |||
| 12 | ISOLOXAPINE | Drug Info | [10] | |||
| 13 | STEPHOLIDINE | Drug Info | [11] | |||
| Antagonist | [+] 4 Antagonist drugs | + | ||||
| 1 | LE-300 | Drug Info | [3] | |||
| 2 | GMC-283 | Drug Info | [3] | |||
| 3 | SKF-83556 | Drug Info | [4] | |||
| 4 | [125I]SCH23982 | Drug Info | [12] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | ZD-3638 | Drug Info | [3] | |||
| Agonist | [+] 3 Agonist drugs | + | ||||
| 1 | (+)-ADTN | Drug Info | [4] | |||
| 2 | beta-ergocriptine | Drug Info | [4] | |||
| 3 | N-propylnorapomorphine | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "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 | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | cAMP signaling pathway | |||||
| 3 | Neuroactive ligand-receptor interaction | |||||
| 4 | Dopaminergic synapse | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Dopamine receptor mediated signaling pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Dopamine receptors | |||||
| 2 | G alpha (s) signalling events | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | Monoamine GPCRs | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | 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 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
| REF 4 | Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. Nature. 1991 Apr 18;350(6319):614-9. | |||||
| REF 5 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
| REF 6 | 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 7 | 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 8 | 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 9 | Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. J Med Chem. 1980 Jun;23(6):635-43. | |||||
| REF 10 | 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 11 | Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities Bioorg Med Chem. 2009 Oct 1;17(19):6898-907. | |||||
| REF 12 | 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. (Target id: 218). | |||||
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