DDRInhibitor是一种高效的盘状结构域受体(discoidindomainreceptor)抑制剂，对DDR2的IC50值为3.3nM，在浓度为1.5nM时，对DDR1有53%的抑制作用。
DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
DDR Inhibitor (Example 6) is a potent DDR inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM[1].
[1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs)
Kinase experiment: | Europium Kinase binding assay is used. Compounds (DDR Inhibitor, etc.) are incubated with 0.5 nM DDR1 or 0.25 nM DDR2 for 1 hour at room temperature in low volume black 384 well assay plates containing 5 nM or 10 nM Kinase Tracer 178 respectively and 2 nM Europium labelled anti-GST antibody in assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA and 0.01 % BRIJ35). The ratio of fluorescence emission 665 nm/615 nm after excitation at 340 nm is obtained. IC50 values are determined from dose-response plots using nonlinear least-squares analysis[1]. |
参考文献: [1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs) | |
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