5WEV

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model

5WEV の概要

• エントリーDOI: 10.2210/pdb5wev/pdb
• 分子名称: Tyrosine-protein kinase JAK2, N-[2-(2,6-dichlorophenyl)-1H-imidazo[4,5-c]pyridin-4-yl]cyclopropanecarboxamide (3 entities in total)
• 機能のキーワード: jak2, kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Endomembrane system ; Peripheral membrane protein : O60674
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 37722.54

構造登録者

Ultsch, M.H.,Magnuson, S. (登録日: 2017-07-10, 公開日: 2017-09-06, 最終更新日: 2023-11-15)

• 主引用文献: Liang, J.,Van Abbema, A.,Balazs, M.,Barrett, K.,Berezhkovsky, L.,Blair, W.S.,Chang, C.,Delarosa, D.,DeVoss, J.,Driscoll, J.,Eigenbrot, C.,Goodacre, S.,Ghilardi, N.,MacLeod, C.,Johnson, A.,Bir Kohli, P.,Lai, Y.,Lin, Z.,Mantik, P.,Menghrajani, K.,Nguyen, H.,Peng, I.,Sambrone, A.,Shia, S.,Smith, J.,Sohn, S.,Tsui, V.,Ultsch, M.,Williams, K.,Wu, L.C.,Yang, W.,Zhang, B.,Magnuson, S.; Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.; Bioorg. Med. Chem. Lett., 27:4370-4376, 2017; PubMed: 28830649; DOI: 10.1016/j.bmcl.2017.08.022

実験手法

X-RAY DIFFRACTION (1.854 Å)