2oj9

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2oj9, resolution 2.00Å

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Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor

Overview

The discovery and synthesis of, 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like, growth factor 1-receptor (IGF-1R) are presented. Installing amine, containing side chains at the 4-position of pyridone ring significantly, improved the enzyme potency. SAR and biological activity of these, compounds is presented.

About this Structure

2OJ9 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 Full crystallographic information is available from OCA.

Reference

Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R)., Velaparthi U, Wittman M, Liu P, Stoffan K, Zimmermann K, Sang X, Carboni J, Li A, Attar R, Gottardis M, Greer A, Chang CY, Jacobsen BL, Sack JS, Sun Y, Langley DR, Balasubramanian B, Vyas D, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. Epub 2007 Feb 4. PMID:17317169

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