4YKN

Pi3K alpha lipid kinase with Active Site Inhibitor

Summary for 4YKN

Entry DOI	10.2210/pdb4ykn/pdb
Descriptor	Phosphatidylinositol 3-kinase regulatory subunit alpha,Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform fusion protein, 3-(6-methoxypyridin-3-yl)-5-[({4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfamoyl]phenyl}amino)methyl]benzoic acid (3 entities in total)
Functional Keywords	"lipid kinase", inhibitor, complex, pi3k, pi3k alpha, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (Human) More
Total number of polymer chains	1
Total formula weight	163380.02
Authors	Elkins, P.A. (deposition date: 2015-03-04, release date: 2015-06-17, Last modification date: 2024-02-28)
Primary citation	Yang, H.,Medeiros, P.F.,Raha, K.,Elkins, P.,Lind, K.E.,Lehr, R.,Adams, N.D.,Burgess, J.L.,Schmidt, S.J.,Knight, S.D.,Auger, K.R.,Schaber, M.D.,Franklin, G.J.,Ding, Y.,DeLorey, J.L.,Centrella, P.A.,Mataruse, S.,Skinner, S.R.,Clark, M.A.,Cuozzo, J.W.,Evindar, G. Discovery of a Potent Class of PI3K alpha Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT). Acs Med.Chem.Lett., 6:531-536, 2015 Cited by PubMed: 26005528 DOI: 10.1021/acsmedchemlett.5b00025 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.9 Å)

Structure validation