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烟云听雨铁杆木虫 (正式写手)
金虫
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[求助]
求翻译一段英文文献（药化）
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Three potent Sig-R binding compounds—10{20}, 10{22}, and 10{7} (which contains two basic nitrogen atoms)—were evaluated for their GPCR selectivity against 38 targets, and the results were incorporated in Table 1 (see SI Appendix for a heat map– formatted selectivity table). The three compounds displayed >86∶1 selectivities for the limited number of receptors for which binding was observed at all; an impressive result for compounds obtained in such an abbreviated structure-activity optimization exercise. The N-propyl derivative 10{22}, designed to eliminate binding arising from a pendant aryl-containing side chain, was particularly selective. Here, the only non-Sig-R binding was detected against the 5HT1A receptor (Ki ¼ 4;500 nM) as opposed to Sig-R 1 and Sig-R 2 (Ki values of 12 and 288 nM, respectively), |
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