Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T97613 | ||||
Target Name | Melatonin receptor type 1A (MTNR1A) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Ramelteon | Drug Info | Ki = 14 nM | [7] | |
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [5] | ||
5-methoxycarbonylamino-N-acetyltryptamine | Drug Info | IC50 = 100 nM | [2] | ||
Beta,beta-dimethylmelatonin | Drug Info | Ki = 1.12 nM | [1] | ||
Beta-methylmelatonin | Drug Info | Ki = 1.67 nM | [1] | ||
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide | Drug Info | Ki = 5350 nM | |||
N-(2,3-Dihydro-1H-phenalen-2-yl)-acetamide | Drug Info | Ki = 195 nM | [6] | ||
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide | Drug Info | IC50 = 0.6 nM | [2] | ||
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide | Drug Info | Ki = 1280 nM | [4] | ||
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 183 nM | [4] | ||
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 379 nM | [4] | ||
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide | Drug Info | Ki = 230 nM | [3] | ||
N-(3-(3-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 23.3 nM | [4] | ||
N-(3-(3-methoxyphenyl)propyl)propionamide | Drug Info | Ki = 85.4 nM | [4] | ||
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide | Drug Info | Ki = 257 nM | [4] | ||
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide | Drug Info | Ki = 400 nM | [4] | ||
N-acetylserotonin | Drug Info | Ki = 1640 nM | [6] | ||
UCM-454 | Drug Info | Ki = 1.4 nM | [3] | ||
References | |||||
REF 1 | 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 2 | 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 3 | 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 4 | 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 5 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | ||||
REF 6 | Synthesis of 2-amido-2,3-dihydro-1H-phenalene derivatives as new conformationally restricted ligands for melatonin receptors. J Med Chem. 1996 Aug 2;39(16):3089-95. | ||||
REF 7 | Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.