4PP7

Highly Potent and Selective 3-N-methylquinazoline-4(3H)-one Based Inhibitors of B-RafV600E Kinase

Summary for 4PP7

Entry DOI	10.2210/pdb4pp7/pdb
Descriptor	Serine/threonine-protein kinase B-raf, N-{2,4-difluoro-3-[methyl(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}propane-1-sulfonamide (2 entities in total)
Functional Keywords	serine/threonine-protein kinase b-raf, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (human)
Cellular location	Nucleus (By similarity): P15056
Total number of polymer chains	2
Total formula weight	71280.16
Authors	Wenglowsky, S.,Ren, L.,Grina, J.,Hansen, J.D.,Laird, E.R.,Moreno, D.,Dinkel, V.,Gloor, S.L.,Hastings, G.,Rana, S.,Rasor, K.,Sturgis, H.L.,Voegtli, W.C.,Vigers, G.P.A.,Willis, B.,Mathieu, S.,Rudolph, J. (deposition date: 2014-02-26, release date: 2014-04-09, Last modification date: 2024-02-28)
Primary citation	Wenglowsky, S.,Ren, L.,Grina, J.,Hansen, J.D.,Laird, E.R.,Moreno, D.,Dinkel, V.,Gloor, S.L.,Hastings, G.,Rana, S.,Rasor, K.,Sturgis, H.L.,Voegtli, W.C.,Vigers, G.,Willis, B.,Mathieu, S.,Rudolph, J. Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase. Bioorg.Med.Chem.Lett., 24:1923-1927, 2014 Cited by PubMed: 24675381 DOI: 10.1016/j.bmcl.2014.03.007 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (3.4 Å)

Structure validation