The influence of lead discovery strategies on the properties of drug candidates

Autor:	György M. Keserü, Gergely M. Makara
Rok vydání:	2009
Předmět:	Pharmacology Drug Drug discovery media_common.quotation_subject Nanotechnology General Medicine medicine.disease Clinical trial Lead (geology) Risk analysis (engineering) Lipophilic efficiency Drug Discovery medicine Attrition media_common
Zdroj:	Nature Reviews Drug Discovery. 8:203-212
ISSN:	1474-1784 1474-1776
DOI:	10.1038/nrd2796
Popis:	By analysing the physicochemical properties of a database of hits and leads, Keseru and Makara conclude that high-throughput screening, as well as hit-to-lead optimization practices in general, are responsible for the unfavourable physicochemical profile of recent leads and clinical candidates. Major adjustments may be needed to enable a balanced lead-evolution process and reduce the likelihood of high compound-related attrition in clinical trials.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0a076c632ec00a768a49f4078e61bc7d https://doi.org/10.1038/nrd2796 Zobrazit plný text záznamu Plný text ve formátu PDF