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TAK-615是一种LPA1受体的负变构调节剂(NAM),用于研究肺纤维化。TAK-615高亲和力结合LPA1受体(Kd高亲和力为1.7nM,Kd低亲和力为14.5nM)。
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM)[1].
TAK-615 partially inhibits the LPA response (60% at 10 µM, IC50 of 91±30 nM)[1].
[1]. Jonathan Ellery, et al. Identification of Compounds Acting as Negative Allosteric Modulators of the LPA 1 Receptor. Eur J Pharmacol. 2018 Aug 15;833:8-15.
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