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基于靶点的药物筛选

GPCR|激酶筛选服务|靶点筛选|离子通道服务|药物筛选
爱思益普基于靶点的化合物筛选服务,中枢神经系统和心血管系统化合物筛选服务,技术特色为离子通道靶点的化合物发现和安全性评价服务。欢迎咨询010-67809840。
详细信息

爱思益普已建立了400+激酶


我们的优势:

  • 激酶种类多:目前已建成激酶库超过400个并不断扩大,覆盖常用酪氨酸激酶及常见突变激酶; 

  • 检测准确:对于已有明确特异抑制剂的激酶选用其特异性抑制剂建立试验模型,控制IC50差异与文献报道值在5倍以内,最大不超过七倍; 

  • 检测周期短:化合物检测出报告周期3-5个工作日,1-2个工作日可提交数据;

  • 检测方法:TR-FRET(LANCE Ultra, LathaScreen, HTRF),荧光法(Kinase-Glo, ADP-Glo),Z`-LYTE,Binding assay等。


爱思益普已建立的激酶列表

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部分验证数据(需要更多验证数据请联系我们)



参考文献:


[1]. SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep;64(4):723-32.

[2]. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577.

[3].Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34.

[4]. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.

[5]. Peng SB, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry, 2005, 44(7), 2293-2304.