1224514-70-8Relevant articles and documents
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors
Liang, Jun,Labadie, Sharada,Zhang, Birong,Ortwine, Daniel F.,Patel, Snahel,Vinogradova, Maia,Kiefer, James R.,Mauer, Till,Gehling, Victor S.,Harmange, Jean-Christophe,Cummings, Richard,Lai, Tommy,Liao, Jiangpeng,Zheng, Xiaoping,Liu, Yichin,Gustafson, Amy,Van der Porten, Erica,Mao, Weifeng,Liederer, Bianca M.,Deshmukh, Gauri,An, Le,Ran, Yingqing,Classon, Marie,Trojer, Patrick,Dragovich, Peter S.,Murray, Lesley
supporting information, p. 2974 - 2981 (2017/05/31)
A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed to improve potency, and synthesis of
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors
Chappie, Thomas A.,Humphrey, John M.,Allen, Martin P.,Estep, Kimberly G.,Fox, Carol B.,Lebel, Lorraine A.,Liras, Spiros,Marr, Eric S.,Menniti, Frank S.,Pandit, Jayvardhan,Schmidt, Christopher J.,Tu, Meihua,Williams, Robert D.,Yang, Feng V.
, p. 182 - 185 (2007/10/03)
A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal
