5WEV
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model
Summary for 5WEV
Entry DOI | 10.2210/pdb5wev/pdb |
Descriptor | Tyrosine-protein kinase JAK2, N-[2-(2,6-dichlorophenyl)-1H-imidazo[4,5-c]pyridin-4-yl]cyclopropanecarboxamide (3 entities in total) |
Functional Keywords | jak2, kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Endomembrane system ; Peripheral membrane protein : O60674 |
Total number of polymer chains | 1 |
Total formula weight | 37722.54 |
Authors | Ultsch, M.H.,Magnuson, S. (deposition date: 2017-07-10, release date: 2017-09-06, Last modification date: 2023-11-15) |
Primary citation | 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 Cited by PubMed: 28830649DOI: 10.1016/j.bmcl.2017.08.022 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.854 Å) |
Structure validation
Download full validation report