3QCY

Phosphoinositide-Dependent Kinase-1 (PDK1) kinase domain with 4-[2-Amino-6-(3-amino-1H-indazol-6-yl)-4-pyrimidinyl]-N-phenyl-2-morpholinecarboxamide

Summary for 3QCY

• Entry DOI: 10.2210/pdb3qcy/pdb
• Related: 3NUN 3NUS 3NUU 3NUY 3QCQ 3QCS 3QCX 3QD0 3QD3 3QD4
• Descriptor: 3-phosphoinositide-dependent protein kinase 1, GLYCEROL, SULFATE ION, ... (5 entities in total)
• Functional Keywords: kinase domain, agc kinase, signal transduction, phosphoinositide, phosphorylation on s241, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: O15530
• Total number of polymer chains: 1
• Total formula weight: 37028.07

Authors

Medina, J.R.,Becker, C.J.,Blackledge, C.W.,Duquenne, C.,Feng, Y.,Grant, S.W.,Heerding, D.,Li, W.H.,Miller, W.H.,Romeril, S.P.,Scherzer, D.,Shu, A.,Bobko, M.A.,Chadderton, A.R.,Dumble, M.,Gradiner, C.M.,Gilbert, S.,Liu, Q.,Rabindran, S.K.,Sudakin, V.,Xiang, H.,Brady, P.G.,Campobasso, N.,Ward, P.,Axten, J.M. (deposition date: 2011-01-17, release date: 2011-03-09, Last modification date: 2024-02-21)

• Primary citation: Medina, J.R.,Becker, C.J.,Blackledge, C.W.,Duquenne, C.,Feng, Y.,Grant, S.W.,Heerding, D.,Li, W.H.,Miller, W.H.,Romeril, S.P.,Scherzer, D.,Shu, A.,Bobko, M.A.,Chadderton, A.R.,Dumble, M.,Gardiner, C.M.,Gilbert, S.,Liu, Q.,Rabindran, S.K.,Sudakin, V.,Xiang, H.,Brady, P.G.,Campobasso, N.,Ward, P.,Axten, J.M.; Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors.; J.Med.Chem., 54:1871-1895, 2011; PubMed: 21341675; DOI: 10.1021/jm101527u

Experimental method

X-RAY DIFFRACTION (2.2 Å)