## Abstract For Abstract see ChemInform Abstract in Full Text.
Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1
✍ Scribed by Toshiki Murata; Mitsuyuki Shimada; Sachiko Sakakibara; Takashi Yoshino; Hiroshi Kadono; Tsutomu Masuda; Makoto Shimazaki; Takuya Shintani; Kinji Fuchikami; Katsuya Sakai; Hisayo Inbe; Keisuke Takeshita; Toshiro Niki; Masaomi Umeda; Kevin B. Bacon; Karl B. Ziegelbauer; Timothy B. Lowinger
- Book ID
- 108477401
- Publisher
- Elsevier Science
- Year
- 2003
- Tongue
- English
- Weight
- 214 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0960-894X
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📜 SIMILAR VOLUMES
A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.
1 (n=1) IKKβ: IC 50 = 0.055 μM TNFα: IC 50 = 0.69 μM (THP-1 cell) 2 (n=2) IKKβ: IC 50 = 0.047 μM TNFα: IC 50 = 1.5 μM ( ) n 3 (R 1 = H) IKKβ IC 50 = 0.20 μM TNFα: IC 50 = 0.69 μM 4 (R 1 = Me) IKKβ IC 50 = 0.33 μM TNFα: IC 50 = 2.4 μM