Therapeutic Targets Database
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TTD Target ID: TTDS00422

Target Information
NameMelatonin receptor type 1B    
Type of targetSuccessful target    
SynonymsMTNR1B    
Mel-1B-R    
Mel1b melatonin receptor    
DiseaseInsomnia    [1]
Drug(s)RamelteonApprovedInsomnia[2]
RamelteonDiscontinuedCircadian rhythm sleep disorder(CRSD)[3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP49286
SequenceMSENGSFANCCEAGGWAVRPGWSGAGSARPSRTPRPPWVAPALSAVLIVTTAVDVVGNLL VILSVLRNRKLRNAGNLFLVSLALADLVVAFYPYPLILVAIFYDGWALGEEHCKASAFVM GLSVIGSVFNITAIAINRYCYICHSMAYHRIYRRWHTPLHICLIWLLTVVALLPNFFVGS LEYDPRIYSCTFIQTASTQYTAAVVVIHFLLPIAVVSFCYLRIWVLVLQARRKAKPESRL CLKPSDLRSFLTMFVVFVIFAICWAPLNCIGLAVAINPQEMAPQIPEGLFVTSYLLAYFN SCLNAIVYGLLNQNFRREYKRILLALWNPRHCIQDASKGSHAEGLQSPAPPIIGVQHQAD AL
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor5-methoxycarbonylamino-N-acetyltryptamine[4]
IODOMELATONIN[5]
N- (2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide[6]
N- (2-[4]
N- (3-[7]
N- (3-[7]
N- (3-[7]
N- (3-[8]
N- (3-[7]
N- (3-[7]
N- (3-[7]
N- (3-[7]
N- (3-Benzooxazol-7-yl-propyl)-acetamide[9]
N- (3-Benzooxazol-7-yl-propyl)-butyramide[9]
N- (3-Benzooxazol-7-yl-propyl)-propionamide[9]
N-[3- (2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide[9]
UCM-454[8]
beta,beta-dimethylmelatonin[10]
beta-methylmelatonin[10]
AgonistRamelteon[2]
Ramelteon[3]
MultitargetRamelteon[2]
Ramelteon[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Ramelteon for insomnia symptoms in a community sample of adults with generalized anxiety disorder: an open label study. J Clin Sleep Med. 2009 Feb 15;5(1):28-33. To Reference
Ref 2Effects of ramelteon 8 mg on objective sleep latency in adults with chronic insomnia on nights 1 and 2: pooled analysis. Curr Med Res Opin. 2009 May;25(5):1209-13. To Reference
Ref 3Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 4Bioorg 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. To Reference
Ref 5J Med Chem. 2002 Apr 25;45(9):1853-9.Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3). To Reference
Ref 6Bioorg. Med. Chem. Lett. 4(13):1559-1564 (1994) To Reference
Ref 7Bioorg 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. To Reference
Ref 8J 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. To Reference
Ref 9Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists. To Reference
Ref 10J 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. To Reference



 

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