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• W2891335972 abstract "Bruton's tyrosine kinase (BTK) is a promising drug target for the treatment of multiple diseases, such as B-cell malignances, asthma, and rheumatoid arthritis. A series of novel aminotriazines were identified as highly selective inhibitors of BTK by a scaffold-hopping approach. Subsequent SAR studies of this series using two conformationally different BTK proteins, an activated form of BTK and an unactivated form of BTK, led to the discovery of a highly selective BTK inhibitor, 4b. With significant efficacy in models in vivo and good ADME and safety profiles, 4b was advanced into preclinical studies." @default.
• W2891335972 created "2018-09-27" @default.
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• W2891335972 date "2018-09-14" @default.
• W2891335972 modified "2023-09-26" @default.
• W2891335972 title "Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton’s Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis" @default.
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• W2891335972 doi "https://doi.org/10.1021/acs.jmedchem.8b01147" @default.
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