Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00422
Target NameMelatonin receptor type 1B    
Type of TargetSuccessful target    
Drug Potency against TargetRamelteonKi = 112 nM[1]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamideIC50 = 0.7 nM[2]
5-methoxycarbonylamino-N-acetyltryptamineIC50 = 4000 nM[2]
IODOMELATONINKi = 0.16 nM[3]
UCM-454Ki = 0.16 nM[4]
N-(3-(3-methoxyphenyl)propyl)acetamideKi = 0.751 nM[5]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamideKi = 1.59 nM[5]
N-(3-Benzooxazol-7-yl-propyl)-propionamideKi = 1.8 nM[6]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamideKi = 12.6 nM[5]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamideKi = 2.12 nM[5]
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamideKi = 2.3 nM[6]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamideKi = 2.5 nM[4]
beta,beta-dimethylmelatoninKi = 2.75 nM[7]
beta-methylmelatoninKi = 2.94 nM[7]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamideKi = 26.1 nM[5]
N-(3-Benzooxazol-7-yl-propyl)-butyramideKi = 3.7 nM[6]
N-(3-Benzooxazol-7-yl-propyl)-acetamideKi = 4.3 nM[6]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamideKi = 46.2 nM[5]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamideKi = 5350 nM[8]
N-(3-(3-methoxyphenyl)propyl)propionamideKi = 7.07 nM[5]
Ref 1Trends Pharmacol Sci. 2001 Aug;22(8):409-14.Therapeutic opportunities from muscarinic receptor research. To Reference
Ref 2Bioorg 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 3J 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 4J 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 5Bioorg 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 6Bioorg 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 7J 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
Ref 8Bioorg. Med. Chem. Lett. 4(13):1559-1564 (1994) To Reference



 

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