5DGZ

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors

Summary for 5DGZ

Entry DOI	10.2210/pdb5dgz/pdb
Related	5DHJ 5DIA
Descriptor	Serine/threonine-protein kinase pim-1, (2S)-1-(1H-INDOL-3-YL)-3-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}PROPAN-2-AMINE, PHOSPHATE ION, ... (4 entities in total)
Functional Keywords	pim-1, kinase, atp-competitive, structure-based drug design, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (Human)
Cellular location	Isoform 2: Cytoplasm. Isoform 1: Cell membrane: P11309
Total number of polymer chains	1
Total formula weight	35034.56
Authors	Murray, J.M.,Wallweber, H.,Steffek, M. (deposition date: 2015-08-29, release date: 2015-10-28, Last modification date: 2024-03-06)
Primary citation	Hu, H.,Wang, X.,Chan, G.K.,Chang, J.H.,Do, S.,Drummond, J.,Ebens, A.,Lee, W.,Ly, J.,Lyssikatos, J.P.,Murray, J.,Moffat, J.G.,Chao, Q.,Tsui, V.,Wallweber, H.,Kolesnikov, A. Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors. Bioorg.Med.Chem.Lett., 25:5258-5264, 2015 Cited by PubMed: 26459208 DOI: 10.1016/j.bmcl.2015.09.052 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.502 Å)

Structure validation