An improved model for fragment-based lead generation at AstraZeneca
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- 作者：Nathan Fuller1 ; 5 ; nathan@rodintherapeutics.com" class="auth_mail" title="E-mail the corresponding authorAuthor Vitae ; Loredana Spadola2 ; 5 ; loredana.spadola@astrazeneca.com" class="auth_mail" title="E-mail the corresponding authorAuthor Vitae ; Scott Cowen1 ; Joe Patel1Author Vitae ; Heike Schö ; nherr1 ; Qing Cao1 ; Andrew McKenzie1 ; 6 ; Fredrik Edfeldt3 ; Al Rabow4 ; Robert Goodnow1
- 刊名：Drug Discovery Today
- 出版年：2016
- 出版时间：August 2016
- 年：2016
- 卷：21
- 期：8
- 页码：1272-1283
- 全文大小：1701 K
文摘
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AZ fragment libraries designed for primary screening techniques, X-ray, NMR and SPR.
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Planar and 3D fragments are shown to be complementary in exploring binding pockets.
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49% of all fragment hits at AZ from 2012 to 2015 have been 3D in nature (PBF >0.25).
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The proportion of 3D hits for PPI targets and all other target classes is the same.