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Utilizing the Combination of Binding Kinetics and Micro-Pharmacokinetics Link in Vitro α-Glucosidase Inhibition to in Vivo Target Occupancy

Many compounds with good inhibitory activity (i.e., high affinity) within in vitro experiments failed in vivo studies due to a lack of efficacy from limited target occupancy (TO) in the drug discovery process. Recently, it was found that rate constants of the formation and dissociation of the binary...

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Detalles Bibliográficos
Autores principales: Wang, Guopeng, Ji, Yanhua, Li, Xueyan, Wang, Qian, Gong, Hang, Wang, Baoshun, Liu, Yang, Pan, Yanli
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6770063/
https://www.ncbi.nlm.nih.gov/pubmed/31527517
http://dx.doi.org/10.3390/biom9090493