3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3β |
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| Authors: | Michael Arnost Al Pierce Ernst ter Haar David Lauffer Jaren Madden Kirk Tanner Jeremy Green |
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| Institution: | Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA |
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| Abstract: | A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3β was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit. |
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