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: 26438154 DOI: 10.1158/1535-7163.MCT-15-0539 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.264 Å)

Structure validation