4M7I
Crystal Structure of GSK6157 Bound to PERK (R587-R1092, delete A660-T867) at 2.34A Resolution
Summary for 4M7I
Entry DOI | 10.2210/pdb4m7i/pdb |
Related | 3QD2 4G31 4G34 |
Descriptor | Eukaryotic translation initiation factor 2-alpha kinase 3, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-1H-indol-1-yl]-2-(6-methylpyridin-2-yl)ethanone (3 entities in total) |
Functional Keywords | deletion mutant, catalytic domain, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) More |
Cellular location | Endoplasmic reticulum membrane; Single-pass type I membrane protein: Q9NZJ5 |
Total number of polymer chains | 1 |
Total formula weight | 35211.65 |
Authors | Gampe, R.T.,Axten, J.M. (deposition date: 2013-08-12, release date: 2014-09-03, Last modification date: 2023-09-20) |
Primary citation | Axten, J.M.,Romeril, S.P.,Shu, A.,Ralph, J.,Medina, J.R.,Feng, Y.,Li, W.H.H.,Grant, S.W.,Heerding, D.A.,Minthorn, E.,Mencken, T.,Gaul, N.,Goetz, A.,Stanley, T.,Hassell, A.M.,Gampe, R.T.,Atkins, C.,Kumar, R. Discovery of 5-{4-fluoro-1-[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1H-indol-5-yl}-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2656157), a Potent and Selective PERK Inhibitor Selected for Preclinical Development To be Published, |
Experimental method | X-RAY DIFFRACTION (2.34 Å) |
Structure validation
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