5TO8
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency
Summary for 5TO8
Entry DOI | 10.2210/pdb5to8/pdb |
Descriptor | Protein-tyrosine kinase 2-beta, 25-(methylsulfonyl)-8-(trifluoromethyl)-5,17,18,21,22,23,24,25-octahydro-12H-7,11-(azeno)-16,13-(metheno)pyrido[3,2-i]pyrrolo[1,2-q][1,3,7,11,17]pentaazacyclohenicosin-20(6H)-one (3 entities in total) |
Functional Keywords | kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm: Q14289 |
Total number of polymer chains | 1 |
Total formula weight | 33141.33 |
Authors | Newby, Z.E. (deposition date: 2016-10-17, release date: 2016-12-21, Last modification date: 2024-03-06) |
Primary citation | Farand, J.,Mai, N.,Chandrasekhar, J.,Newby, Z.E.,Van Veldhuizen, J.,Loyer-Drew, J.,Venkataramani, C.,Guerrero, J.,Kwok, A.,Li, N.,Zherebina, Y.,Wilbert, S.,Zablocki, J.,Phillips, G.,Watkins, W.J.,Mourey, R.,Notte, G.T. Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency. Bioorg. Med. Chem. Lett., 26:5926-5930, 2016 Cited by PubMed: 27876318DOI: 10.1016/j.bmcl.2016.10.092 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.9849 Å) |
Structure validation
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