| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T09572 | ||||
| Target Name | Melanin-concentrating hormone receptor 1 (MCHR1) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | AMG 076 | Drug Info | IC50 = 0.9~24 nM | [9] | |
| NGD-4715 | Drug Info | IC50 = 0.9~24 nM | [9] | ||
| T-226296 | Drug Info | IC50 = 5.5 nM | [11] | ||
| 2-phenyl-N,N-bis(o-tolylthiomethyl)ethanamine | Drug Info | Ki = 7500 nM | [8] | ||
| 8-(1,2-Dimethyl-propoxy)-quinolin-2-ylamine | Drug Info | IC50 = 199 nM | [1] | ||
| 8-(1,3,3-Trimethyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 210 nM | [2] | ||
| 8-(1-Ethyl-propoxy)-quinolin-2-ylamine | Drug Info | IC50 = 326 nM | [1] | ||
| 8-(1-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 860 nM | [1] | ||
| 8-(2-Cyclopropyl-ethoxy)-quinolin-2-ylamine | Drug Info | IC50 = 492 nM | [1] | ||
| 8-(2-Ethoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | IC50 = 1070 nM | [1] | ||
| 8-(2-Ethyl-1-methyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 1300 nM | [1] | ||
| 8-(2-Methoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | IC50 = 606 nM | [1] | ||
| 8-(2-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 36 nM | [1] | ||
| 8-(2-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | IC50 = 1330 nM | [1] | ||
| 8-(3,3,3-trifluoropropoxy)quinolin-2-amine | Drug Info | IC50 = 722 nM | [1] | ||
| 8-(3,3-Dimethyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 201 nM | [1] | ||
| 8-(3-Methoxy-3-methyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 132 nM | [1] | ||
| 8-(3-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | IC50 = 614 nM | [1] | ||
| 8-(3-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | IC50 = 640 nM | [1] | ||
| 8-(3-Methyl-cyclopentyloxy)-quinolin-2-ylamine | Drug Info | IC50 = 823 nM | [1] | ||
| 8-(4-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | IC50 = 349 nM | [1] | ||
| 8-Butoxy-quinolin-2-ylamine | Drug Info | IC50 = 789 nM | [1] | ||
| 8-Cyclobutylmethoxy-quinolin-2-ylamine | Drug Info | IC50 = 432 nM | [1] | ||
| 8-Cycloheptyloxy-quinolin-2-ylamine | Drug Info | IC50 = 3480 nM | [1] | ||
| 8-Cyclohexyloxy-quinolin-2-ylamine | Drug Info | IC50 = 361 nM | [1] | ||
| 8-Cyclopentylmethoxy-quinolin-2-ylamine | Drug Info | IC50 = 2290 nM | [1] | ||
| 8-Hexyloxy-quinolin-2-ylamine | Drug Info | IC50 = 818 nM | [1] | ||
| 8-Isopropoxy-quinolin-2-ylamine | Drug Info | IC50 = 437 nM | [1] | ||
| 8-Methoxy-quinolin-2-ylamine | Drug Info | IC50 = 1590 nM | [1] | ||
| 8-Pentyloxy-quinolin-2-ylamine | Drug Info | IC50 = 580 nM | [1] | ||
| 8-Propoxy-quinolin-2-ylamine | Drug Info | IC50 = 1100 nM | [1] | ||
| 8-sec-Butoxy-quinolin-2-ylamine | Drug Info | IC50 = 5310 nM | [1] | ||
| A-224940 | Drug Info | IC50 = 1680 nM | [3] | ||
| ADS-102891 | Drug Info | IC50 = 100 nM | [7] | ||
| ADS-103168 | Drug Info | IC50 = 9 nM | [7] | ||
| ADS-103214 | Drug Info | IC50 = 9 nM | [7] | ||
| ADS-103253 | Drug Info | IC50 = 58 nM | [7] | ||
| ADS-103254 | Drug Info | IC50 = 164 nM | [7] | ||
| ADS-103274 | Drug Info | IC50 = 28 nM | [7] | ||
| ADS-103293 | Drug Info | IC50 = 1930 nM | [7] | ||
| ADS-103294 | Drug Info | IC50 = 101 nM | [7] | ||
| ADS-103316 | Drug Info | IC50 = 41 nM | [7] | ||
| AR-129330 | Drug Info | IC50 = 7.2 nM | [10] | ||
| GNF-PF-1550 | Drug Info | IC50 = 16 nM | [4] | ||
| N,N-bis(tosylmethyl)hexan-1-amine | Drug Info | Ki = 1700 nM | [8] | ||
| N-(1-benzylpiperidin-4-yl)-3,5-dimethoxybenzamide | Drug Info | Ki = 302 nM | [5] | ||
| N-(4-amino-2-propylquinolin-6-yl)cinnamamide | Drug Info | IC50 = 1000 nM | [6] | ||
| Phenyl-N,N-bis(tosylmethyl)methanamine | Drug Info | Ki = 7500 nM | [8] | ||
| Action against Disease Model | AMG 076 | Drug Info | MCH-1R antagonists such as GW856464,AMG-07619 and and NGD-4715 produced anti-obese effects in diet-induced obese (DIO) rats | [9] | |
| References | |||||
| REF 1 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4873-7. | ||||
| REF 2 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4879-82. | ||||
| REF 3 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4883-6. | ||||
| REF 4 | 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and ... J Med Chem. 2005 Sep 8;48(18):5684-97. | ||||
| REF 5 | Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5445-50. | ||||
| REF 6 | 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. | ||||
| REF 7 | Quinazoline and benzimidazole MCH-1R antagonists. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. | ||||
| REF 8 | Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening. J Med Chem. 2008 Feb 14;51(3):581-8. | ||||
| REF 9 | Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5339-45. | ||||
| REF 10 | Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. | ||||
| REF 11 | The medicinal chemistry of agents targeting monoacylglycerol lipase. Curr Top Med Chem. 2008;8(3):231-46. | ||||
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