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6N3L

Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents

Summary for 6N3L
Entry DOI10.2210/pdb6n3l/pdb
DescriptoreIF-2-alpha kinase GCN2,eIF-2-alpha kinase GCN2, N-{6-[(1-methyl-2-{[4-(trifluoromethyl)phenyl]amino}-1H-benzimidazol-5-yl)oxy]pyrimidin-4-yl}cyclopropanecarboxamide (3 entities in total)
Functional Keywordsgcn2, kinase, inhibitor, anti-tumor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
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Total number of polymer chains2
Total formula weight76638.10
Authors
Hoffman, I.D.,Fujimoto, J.,Kurasawa, O.,Takagi, T.,Klein, M.G.,Kefala, G.,Ding, S.C.,Cary, D.R.,Mizojiri, R. (deposition date: 2018-11-15, release date: 2019-10-09, Last modification date: 2024-03-13)
Primary citationFujimoto, J.,Kurasawa, O.,Takagi, T.,Liu, X.,Banno, H.,Kojima, T.,Asano, Y.,Nakamura, A.,Nambu, T.,Hata, A.,Ishii, T.,Sameshima, T.,Debori, Y.,Miyamoto, M.,Klein, M.G.,Tjhen, R.,Sang, B.C.,Levin, I.,Lane, S.W.,Snell, G.P.,Li, K.,Kefala, G.,Hoffman, I.D.,Ding, S.C.,Cary, D.R.,Mizojiri, R.
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Acs Med.Chem.Lett., 10:1498-1503, 2019
Cited by
PubMed: 31620240
DOI: 10.1021/acsmedchemlett.9b00400
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.61 Å)
Structure validation

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