PDBsum entry 2wqb

Transferase

PDB id: 2wqb

Contents

Protein chain

289 a.a.

Ligands

QQ1

Waters ×19

References listed in PDB file

Key reference

• Title: Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against tie-2 in vitro and in vivo.
• Authors: R.W.Luke, P.Ballard, D.Buttar, L.Campbell, J.Curwen, S.C.Emery, A.M.Griffen, L.Hassall, B.R.Hayter, C.D.Jones, W.Mccoull, M.Mellor, M.L.Swain, J.A.Tucker.
• Ref.: Bioorg Med Chem Lett, 2009, 19, 6670-6674.
• PubMed id: 19854647

Abstract

The SAR and improvement in potency against Tie2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. The crystal structure of one of these compounds bound to the Tie-2 kinase domain is consistent with the SAR. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2.