2. Academic Validation
  3. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2

The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2

  • Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70. doi: 10.1016/s0960-894x(03)00058-1.
Josie A Blackie 1,  Jackie C Bloomer,  Murray J B Brown,  Hung Yuan Cheng,  Beverley Hammond,  Deirdre M B Hickey,  Robert J Ife,  Colin A Leach,  V Ann Lewis,  Colin H Macphee,  Kevin J Milliner,  Kitty E Moores,  Ivan L Pinto,  Stephen A Smith,  Ian G Stansfield,  Steven J Stanway,  Maxine A Taylor,  Colin J Theobald
Affiliations

Affiliation

  • 1 Medicines Research Centre, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, UK.
PMID: 12643913 DOI: 10.1016/s0960-894x(03)00058-1
Abstract

Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated Phospholipase A(2) with sub-nanomolar potency. Cyclopentyl fused derivative 21, SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man.

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