Challenges in the Medicinal Chemical Optimization of Binding Kinetics

التفاصيل البيبلوغرافية
العنوان: Challenges in the Medicinal Chemical Optimization of Binding Kinetics
المؤلفون: Waring, Michael J., Leach, Andrew G., Miller, Duncan C.
المصدر: Waring , M J , Leach , A G & Miller , D C 2015 , Challenges in the Medicinal Chemical Optimization of Binding Kinetics . in Thermodynamics and Kinetics of Drug Binding . John Wiley & Sons Ltd , pp. 191-210 . https://doi.org/10.1002/9783527673025.ch10Test
بيانات النشر: John Wiley & Sons Ltd
سنة النشر: 2015
المجموعة: The University of Manchester: Research Explorer - Publications
مصطلحات موضوعية: Binding kinetics, Medicinal chemistry optimisation, Residence time, Structure-kinetic relationships
الوصف: This chapter describes the key considerations and challenges to optimizing binding kinetics. The challenges relate both to our ability to measure on and off rates in a manner that informs optimization but also in our limited molecular understanding of the processes that govern on and off rates. The effects of individual molecular interactions and bulk physicochemical properties are discussed. A number of significant case studies from the literature are described, which serve to highlight these principles. These examples also illustrate that empirical optimization of residence time is possible if given adequate attention during optimization and that some of the principles discussed may have general applicability.
نوع الوثيقة: book part
اللغة: English
DOI: 10.1002/9783527673025.ch10
الإتاحة: https://doi.org/10.1002/9783527673025.ch10Test
https://research.manchester.ac.uk/en/publications/1799a53e-ad2a-4b8b-8fb8-b60005352d91Test
http://www.scopus.com/inward/record.url?scp=84979719172&partnerID=8YFLogxKTest
حقوق: info:eu-repo/semantics/restrictedAccess
رقم الانضمام: edsbas.E927D8B8
قاعدة البيانات: BASE