1oit | pdb_00001oit

IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION

File:1oit.gif

spinqualitylabelsall models 1oit, resolution 1.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D

Overview

High-throughput screening identified the imidazo[1,2-a]pyridine and, bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase, CDK4. Comparison of their experimentally-determined binding modes and, emerging structure-activity trends led to the development of potent and, selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular, CDK2.

About this Structure

1OIT is a [Single protein] structure of sequence from [Homo sapiens] with HDT as [ligand]. Active as [[1]], with EC number [2.7.1.37]. Full crystallographic information is available from [OCA].

Reference

Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation., Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ, Bioorg Med Chem Lett. 2003 Sep 15;13(18):3021-6. PMID:12941325

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