5TC0

Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate

Summary for 5TC0

• Entry DOI: 10.2210/pdb5tc0/pdb
• Descriptor: Tyrosine-protein kinase Mer, N-(2-{4-[(2S)-4-(methylsulfonyl)morpholin-2-yl]-1,3-thiazol-2-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: 72422.61

Authors

Hoffman, I.D.,Lawson, J.D. (deposition date: 2016-09-13, 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; PubMed: 28082036; DOI: 10.1016/j.bmcl.2016.12.024

Experimental method

X-RAY DIFFRACTION (2.24 Å)