2. Academic Validation
  3. Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors

Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors

  • Bioorg Med Chem Lett. 2004 Jun 7;14(11):2817-22. doi: 10.1016/j.bmcl.2004.03.058.
Andrew Baxter 1,  Steve Brough,  Anne Cooper,  Eike Floettmann,  Steve Foster,  Christine Harding,  Jason Kettle,  Tom McInally,  Craig Martin,  Michelle Mobbs,  Maurice Needham,  Pete Newham,  Stuart Paine,  Steve St-Gallay,  Sylvia Salter,  John Unitt,  Yafeng Xue
Affiliations

Affiliation

  • 1 AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. [email protected]
PMID: 15125939 DOI: 10.1016/j.bmcl.2004.03.058
Abstract

A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.

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