3V5Q

Discovery of a selective TRK Inhibitor with efficacy in rodent cancer tumor models

Summary for 3V5Q

• Entry DOI: 10.2210/pdb3v5q/pdb
• Descriptor: NT-3 growth factor receptor, CHLORIDE ION, 1-(3-{[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-indol-6-yl]amino}phenyl)-3-[3-(trifluoromethyl)phenyl]urea, ... (4 entities in total)
• Functional Keywords: kinase domain, kinase, phosphorylation, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Membrane; Single-pass type I membrane protein: Q16288
• Total number of polymer chains: 2
• Total formula weight: 68923.39

Authors

Kreusch, A. (deposition date: 2011-12-16, release date: 2012-02-08, Last modification date: 2024-02-28)

• Primary citation: Albaugh, P.,Fan, Y.,Mi, Y.,Sun, F.,Adrian, F.,Li, N.,Jia, Y.,Sarkisova, Y.,Kreusch, A.,Hood, T.,Lu, M.,Liu, G.,Huang, S.,Liu, Z.,Loren, J.,Tuntland, T.,Karanewsky, D.S.,Seidel, H.M.,Molteni, V.; Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.; ACS Med Chem Lett, 3:140-145, 2012; PubMed: 24900443; DOI: 10.1021/ml200261d

Experimental method

X-RAY DIFFRACTION (2.2001 Å)