Target Information
Target General Infomation | |||||
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Target ID |
T48268
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Former ID |
TTDS00422
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Target Name |
Melatonin receptor type 1B
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Gene Name |
MTNR1B
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Synonyms |
Mel-1B-R; Mel1b melatonin receptor; MTNR1B
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Target Type |
Successful
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Disease | Circadian rhythm sleep disorder [ICD9: 327.3, 780.55; ICD10: G47.2] | ||||
Epilepsy [ICD10: G40] | |||||
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0] | |||||
Function |
High affinityreceptor for melatonin. Likely to mediates 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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T48268
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UniProt ID | |||||
Sequence |
MSENGSFANCCEAGGWAVRPGWSGAGSARPSRTPRPPWVAPALSAVLIVTTAVDVVGNLL
VILSVLRNRKLRNAGNLFLVSLALADLVVAFYPYPLILVAIFYDGWALGEEHCKASAFVM GLSVIGSVFNITAIAINRYCYICHSMAYHRIYRRWHTPLHICLIWLLTVVALLPNFFVGS LEYDPRIYSCTFIQTASTQYTAAVVVIHFLLPIAVVSFCYLRIWVLVLQARRKAKPESRL CLKPSDLRSFLTMFVVFVIFAICWAPLNCIGLAVAINPQEMAPQIPEGLFVTSYLLAYFN SCLNAIVYGLLNQNFRREYKRILLALWNPRHCIQDASKGSHAEGLQSPAPPIIGVQHQAD AL |
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Drugs and Mode of Action | |||||
Inhibitor | 5-methoxycarbonylamino-N-acetyltryptamine | Drug Info | [529396] | ||
Beta,beta-dimethylmelatonin | Drug Info | [528234] | |||
Beta-methylmelatonin | Drug Info | [528234] | |||
IODOMELATONIN | Drug Info | [526317] | |||
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide | Drug Info | [551266] | |||
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide | Drug Info | [529396] | |||
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide | Drug Info | [529949] | |||
N-(3-(3-methoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-(3-methoxyphenyl)propyl)propionamide | Drug Info | [530786] | |||
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide | Drug Info | [530786] | |||
N-(3-Benzooxazol-7-yl-propyl)-acetamide | Drug Info | [527111] | |||
N-(3-Benzooxazol-7-yl-propyl)-butyramide | Drug Info | [527111] | |||
N-(3-Benzooxazol-7-yl-propyl)-propionamide | Drug Info | [527111] | |||
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide | Drug Info | [527111] | |||
UCM-454 | Drug Info | [529949] | |||
Modulator | Ramelteon | Drug Info | [529337], [532551] | ||
VLB-01 | Drug Info | [1572591] | |||
Agonist | Tasimelteon | Drug Info | [542414] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 538833 | (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: 1356). | ||||
Ref 542414 | (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: 7393). | ||||
Ref 526317 | J Med Chem. 2002 Apr 25;45(9):1853-9.Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3). | ||||
Ref 527111 | Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists. | ||||
Ref 528234 | J Med Chem. 2006 Jun 15;49(12):3509-19.Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines. | ||||
Ref 529337 | Ramelteon: a melatonin receptor agonist for the treatment of insomnia. J Postgrad Med. 2008 Jan-Mar;54(1):45-8. | ||||
Ref 529396 | Bioorg Med Chem. 2008 May 1;16(9):4954-62. Epub 2008 Mar 17.Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3. | ||||
Ref 529949 | J Med Chem. 2009 Feb 12;52(3):826-33.2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists. | ||||
Ref 530786 | Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. Epub 2010 Feb 25.Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands. | ||||
Ref 532551 | MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85. | ||||
Ref 542414 | (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: 7393). |
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