PDBsum entry 3mpm

Transferase

PDB id: 3mpm

Contents

Protein chain

257 a.a.

Ligands

5LK

EDO

Waters ×258

References listed in PDB file

Key reference

• Title: New pyrazolo[1,5a]pyrimidines as orally active inhibitors of lck.
• Authors: N.Gommermann, P.Buehlmayer, A.Von matt, W.Breitenstein, K.Masuya, B.Pirard, P.Furet, S.W.Cowan-Jacob, G.Weckbecker.
• Ref.: Bioorg Med Chem Lett, 2010, 20, 3628-3631.
• PubMed id: 20483608

Abstract

A novel series of pyrazolo[1,5a]pyrimidines was optimized to target lymphocyte-specific kinase (Lck). An efficient synthetic route was developed and SAR studies toward activity and selectivity are described, leading to Lck inhibitors with enzymatic, cellular and in vivo potency.