Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton’s Tyrosine Kinase

Although Bruton’s tyrosine kinase (BTK) has been recognized as a validated drug target for the treatment of B-cell malignances, the emergence of clinical resistance to the first-generation covalent BTK inhibitors is becoming a serious concern. As a part of our effort to develop noncovalent BTK inhib...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-10, Vol.64 (19), p.14129-14141
Hauptverfasser:	Kawahata, Wataru, Asami, Tokiko, Kiyoi, Takao, Irie, Takayuki, Kashimoto, Shigeki, Furuichi, Hatsuo, Sawa, Masaaki
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Agammaglobulinaemia Tyrosine Kinase - antagonists & inhibitors Agammaglobulinaemia Tyrosine Kinase - metabolism Dose-Response Relationship, Drug Drug Discovery Humans Molecular Structure Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship
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