5TD2
Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate
Summary for 5TD2
Entry DOI | 10.2210/pdb5td2/pdb |
Descriptor | Tyrosine-protein kinase Mer, N-[2-{4-[(2S)-4-(methylsulfonyl)morpholin-2-yl]-1,3-thiazol-2-yl}-4-(morpholin-4-yl)phenyl]-1H-imidazole-2-carboxamide (3 entities in total) |
Functional Keywords | kinase, inhibitor, surrogate, oncology, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Membrane ; Single-pass type I membrane protein : Q12866 |
Total number of polymer chains | 2 |
Total formula weight | 66158.89 |
Authors | Hoffman, I.D.,Lawson, J.D. (deposition date: 2016-09-16, release date: 2017-01-25, Last modification date: 2024-03-06) |
Primary citation | Keung, W.,Boloor, A.,Brown, J.,Kiryanov, A.,Gangloff, A.,Lawson, J.D.,Skene, R.,Hoffman, I.,Atienza, J.,Kahana, J.,De Jong, R.,Farrell, P.,Balakrishna, D.,Halkowycz, P. Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate. Bioorg. Med. Chem. Lett., 27:1099-1104, 2017 Cited by PubMed: 28082036DOI: 10.1016/j.bmcl.2016.12.024 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.68 Å) |
Structure validation
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