The advantages of describing covalent inhibitor in vitro potencies by IC
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 01 2021
01 01 2021
Historique:
received:
25
08
2020
revised:
30
10
2020
accepted:
03
11
2020
pubmed:
8
12
2020
medline:
31
7
2021
entrez:
7
12
2020
Statut:
ppublish
Résumé
Recent years have seen a resurgence in drug discovery efforts aimed at the identification of covalent inhibitors which has led to an explosion of literature reports in this area and most importantly new approved therapies. These reports and breakthroughs highlight the significant investments made across the industry in SAR campaigns to optimize inhibitors. The potency of covalent inhibitors is generally considered to be more accurately described by the time-independent kinetic parameter k
Identifiants
pubmed: 33285410
pii: S0968-0896(20)30695-7
doi: 10.1016/j.bmc.2020.115865
pii:
doi:
Substances chimiques
Protein Kinase Inhibitors
0
Recombinant Proteins
0
JAK3 protein, human
EC 2.7.10.2
Janus Kinase 3
EC 2.7.10.2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115865Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.