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- W2108622527 abstract "SAR studies of a series of piperazinebenzylamines resulted in identification of potent agonists and antagonists of the human melanocortin-4 receptor. Thus, the 1,2,3,4-tetrahydroisoquinolin-1-ylacetyl compound 12e and the quinolin-3-ylcarbonyl analogue 12l possessed K(i) values of 6.3 and 4.5 nM, respectively. Interestingly, 12e was a full agonist with an EC(50) value of 31 nM, and 12l was a weak partial agonist (IA=17%) and functioned as an antagonist (IC(50)=300 nM)." @default.
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- W2108622527 date "2005-02-01" @default.
- W2108622527 modified "2023-09-26" @default.
- W2108622527 title "Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines" @default.
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- W2108622527 doi "https://doi.org/10.1016/j.bmcl.2004.10.096" @default.
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