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Fragment-based lead discovery is establishing itself as valuable approach for the discovery of novel small molecule leads. It relies on establishing a better understanding of the binding mechanism of a ligand for its binding partner by probing for “hot spots “on the protein target with small molecule fragments (typically <300 Daltons). Its simplicity is in the principle of building a pharmacophore from the ground up. Successful selection requires data on binding affinity as well as extensive SAR information provided by a variety of techniques . . .
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• Volume 17 • Issue 1 • January 2021

December 2020/January 2021

December 2020/January 2021 issue