Chemical Biology and Drug Design p. 54 - 65 (2016)
Update date:2022-08-11
Topics:
Vasilevich, Natalya I.
Aksenova, Elena A.
Kazyulkin, Denis N.
Afanasyev, Ilya I.
A general pharmachophore model for various types of Ser/Thr kinases was developed. Search for the molecules fitting to this pharmacophore among ASINEX proprietary library revealed a number of compounds, which were tested and appeared to possess some activity against several Ser/Thr kinases such as Aurora A, Aurora B and Haspin. The possibility of performing the fine-tuning of the general Ser/Thr pharmacophore to desired types of kinase to get active and selective inhibitors was exemplified by Aurora A kinase. As a result, several hits in 3–5?nm range of activity against Aurora A kinase with rather good selectivity and ADME properties were obtained.
View MoreTaixing Joxin Bio-tec Co.,Ltd.
website:http://www.joxbio.com
Contact:86-523-87558858 87612088
Address:No.88, chengdong industrial park
Shenzhen JYMed Technology Co.,Ltd.
website:http://www.jymedtech.com
Contact:+86-755-26612112
Address:RM1-105, Shenzhen Bio-incubator Base, 10 Gaoxin C Avc 1st, Nanshan District, Shenzhen, GD, China, 518057
Shandong Xingshun New Material Co., Ltd.
website:http://www.sd-xingshun.com
Contact:+86-519-86461196/+86-519-86464994
Address:Middle of Luhua East Road, Dingtao District
Shandong Shouguang Songchuan Industrial Additives Co.,Ltd
Contact:+86-536-8566856
Address:Shouguang,Shandong,China
Contact:(86) 731 88718666
Address:Room 1222, Unit 4, Building B, Shangcheng, No.47, Kaiyuan East Road.
Doi:10.1246/bcsj.62.3609
(1989)Doi:10.1016/j.chembiol.2009.12.013
(2010)Doi:10.1016/0040-4039(91)80137-U
(1991)Doi:10.1039/c6cc01730d
(2016)Doi:10.1016/j.apcata.2017.04.012
(2017)Doi:10.1007/BF00995703
(1984)