Target Validation Information
Target ID T48268
Target Name Melatonin receptor type 1B
Target Type
Successful
Drug Potency against Target Ramelteon Drug Info Ki = 112 nM [552263]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide Drug Info Ki = 12.6 nM [530786]
UCM-454 Drug Info Ki = 0.16 nM [529949]
N-(3-(3-methoxyphenyl)propyl)acetamide Drug Info Ki = 0.751 nM [530786]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide Drug Info IC50 = 0.7 nM [529396]
Beta-methylmelatonin Drug Info Ki = 2.94 nM [528234]
Beta,beta-dimethylmelatonin Drug Info Ki = 2.75 nM [528234]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide Drug Info Ki = 46.2 nM [530786]
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide Drug Info Ki = 2.3 nM [527111]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide Drug Info Ki = 26.1 nM [530786]
N-(3-(3-methoxyphenyl)propyl)propionamide Drug Info Ki = 7.07 nM [530786]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide Drug Info Ki = 2.12 nM [530786]
5-methoxycarbonylamino-N-acetyltryptamine Drug Info IC50 = 4000 nM [529396]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide Drug Info Ki = 1.59 nM [530786]
IODOMELATONIN Drug Info Ki = 0.16 nM [526317]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide Drug Info Ki = 2.5 nM [529949]
N-(3-Benzooxazol-7-yl-propyl)-butyramide Drug Info Ki = 3.7 nM [527111]
N-(3-Benzooxazol-7-yl-propyl)-propionamide Drug Info Ki = 1.8 nM [527111]
N-(3-Benzooxazol-7-yl-propyl)-acetamide Drug Info Ki = 4.3 nM [527111]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide Drug Info Ki = 5350 nM
References
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 530786Bioorg 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 529949J 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 530786Bioorg 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 529396Bioorg 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 528234J 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 528234J 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 530786Bioorg 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 527111Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Ref 530786Bioorg 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 530786Bioorg 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 530786Bioorg 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 529396Bioorg 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 530786Bioorg 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 526317J 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 529949J 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 527111Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Ref 527111Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Ref 527111Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.

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