BACE1-IN-4 是一种有效、高度选择性的 BACE1 抑制剂，IC50 值为 3.8 nM，Ki 值为 1.9 nM。抗阿尔滋海默症。
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer's disease[1]. IC50: 3.8 nM (BACE1), 2090 nM (BACE2)[1]Ki: 1.9 nM (BACE1), 1740 nM (BACE2)[1]
BACE1-IN-4 (Compound 22) is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2 (IC50, 2090 nM; Ki, 1740 nM)[1].
[1]. Fujimoto K, et al. Structure-Based Design of Selective β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2. J Med Chem. 2019 May 23;62(10):5080-5095.
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