5AMN

The Discovery of 2-Substituted Phenol Quinazolines as Potent and Selective RET Kinase Inhibitors

Summary for 5AMN

• Entry DOI: 10.2210/pdb5amn/pdb
• Descriptor: PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET, 4-[3-HYDROXYANILINO]-6,7-DIMETHOXYQUINAZOLINE, FORMIC ACID, ... (4 entities in total)
• Functional Keywords: transferase, ret, oncogene, receptor tyrosine kinase, chemical inhibitor, cancer
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Cell membrane ; Single-pass type I membrane protein : P07949
• Total number of polymer chains: 1
• Total formula weight: 34973.10

Authors

Newton, R.,Bowler, K.,Burns, E.M.,Chapman, P.,Fairweather, E.,Fritzl, S.,Goldberg, K.,Hamilton, N.M.,Holt, S.V.,Hopkins, G.V.,Jones, S.D.,Jordan, A.M.,Lyons, A.,McDonald, N.Q.,Maguire, L.A.,Mould, D.P.,Purkiss, A.G.,Small, H.F.,Stowell, A.,Thomson, G.J.,Waddell, I.D.,Waszkowycz, B.,Watson, A.J.,Ogilvie, D.J. (deposition date: 2015-03-11, release date: 2016-02-17, Last modification date: 2024-01-10)

• Primary citation: Newton, R.,Bowler, K.A.,Burns, E.M.,Chapman, P.J.,Fairweather, E.E.,Fritzl, S.J.R.,Goldberg, K.M.,Hamilton, N.M.,Holt, S.V.,Hopkins, G.V.,Jones, S.D.,Jordan, A.M.,Lyons, A.J.,Nikki March, H.,McDonald, N.Q.,Maguire, L.A.,Mould, D.P.,Purkiss, A.G.,Small, H.F.,Stowell, A.I.J.,Thomson, G.J.,Waddell, I.D.,Waszkowycz, B.,Watson, A.J.,Ogilvie, D.J.; The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.; Eur J Med Chem, 112:20-32, 2016; PubMed: 26874741; DOI: 10.1016/j.ejmech.2016.01.039

Experimental method

X-RAY DIFFRACTION (2.57 Å)