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. 2004 Jun 7;14(11):2817-22.
doi: 10.1016/j.bmcl.2004.03.058.

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

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

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

Andrew Baxter et al. Bioorg Med Chem Lett. .

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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