5E1S
The Crystal structure of INSR Tyrosine Kinase in complex with the Inhibitor BI 885578
Summary for 5E1S
Entry DOI | 10.2210/pdb5e1s/pdb |
Descriptor | Insulin receptor, (5R)-N-(1-{2-[4-(2-methoxyethyl)piperazin-1-yl]ethyl}-1H-pyrazol-3-yl)-5,8-dimethyl-9-phenyl-6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine (3 entities in total) |
Functional Keywords | kinase, insr, igf-1r, inhibitor, transferase |
Biological source | Homo sapiens (Human) |
Cellular location | Cell membrane; Single-pass type I membrane protein: P06213 |
Total number of polymer chains | 1 |
Total formula weight | 35479.61 |
Authors | Kessler, D.,Zahn, S.,Sanderson, M.,Wolkerstorfer, B. (deposition date: 2015-09-30, release date: 2015-10-14, Last modification date: 2024-01-10) |
Primary citation | Sanderson, M.P.,Apgar, J.,Garin-Chesa, P.,Hofmann, M.H.,Kessler, D.,Quant, J.,Savchenko, A.,Schaaf, O.,Treu, M.,Tye, H.,Zahn, S.K.,Zoephel, A.,Haaksma, E.,Adolf, G.R.,Kraut, N. BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis. Mol.Cancer Ther., 14:2762-2772, 2015 Cited by PubMed: 26438154DOI: 10.1158/1535-7163.MCT-15-0539 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.264 Å) |
Structure validation
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