Discovery of imidazo[1,2-b]pyridazines as IKKβ inhibitors. Part 2: Improvement of potency in vitro and in vivo

✍ Scribed by Hiroki Shimizu; Isao Yasumatsu; Tomoaki Hamada; Yoshiyuki Yoneda; Tomonori Yamasaki; Shinji Tanaka; Tadashi Toki; Mika Yokoyama; Kaoru Morishita; Shin Iimura

• Book ID: 104005253
• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 796 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.12.078

✦ Synopsis

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