Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T48268 | ||||
Target Name | Melatonin receptor type 1B (MTNR1B) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Ramelteon | Drug Info | Ki = 112 nM | [7] | |
Drug Info | Ki = 0.751 nM | [6] | |||
Drug Info | Ki = 26.1 nM | [6] | |||
Drug Info | Ki = 2.5 nM | [5] | |||
2-iodo-melatonin | Drug Info | Ki = 0.16 nM | [1] | ||
5-methoxycarbonylamino-N-acetyltryptamine | Drug Info | IC50 = 4000 nM | [4] | ||
Beta,beta-dimethylmelatonin | Drug Info | Ki = 2.75 nM | [3] | ||
Beta-methylmelatonin | Drug Info | Ki = 2.94 nM | [3] | ||
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide | Drug Info | Ki = 5350 nM | |||
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide | Drug Info | IC50 = 0.7 nM | [4] | ||
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 1.59 nM | [6] | ||
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 46.2 nM | [6] | ||
N-(3-(3-methoxyphenyl)propyl)propionamide | Drug Info | Ki = 7.07 nM | [6] | ||
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 12.6 nM | [6] | ||
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide | Drug Info | Ki = 2.12 nM | [6] | ||
N-(3-Benzooxazol-7-yl-propyl)-acetamide | Drug Info | Ki = 4.3 nM | [2] | ||
N-(3-Benzooxazol-7-yl-propyl)-butyramide | Drug Info | Ki = 3.7 nM | [2] | ||
N-(3-Benzooxazol-7-yl-propyl)-propionamide | Drug Info | Ki = 1.8 nM | [2] | ||
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide | Drug Info | Ki = 2.3 nM | [2] | ||
UCM-454 | Drug Info | Ki = 0.16 nM | [5] | ||
References | |||||
REF 1 | Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3). J Med Chem. 2002 Apr 25;45(9):1853-9. | ||||
REF 2 | Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802. | ||||
REF 3 | Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-me... J Med Chem. 2006 Jun 15;49(12):3509-19. | ||||
REF 4 | Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3. Bioorg Med Chem. 2008 May 1;16(9):4954-62. | ||||
REF 5 | 2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists. J Med Chem. 2009 Feb 12;52(3):826-33. | ||||
REF 6 | Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. | ||||
REF 7 | Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14. | ||||
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