Abstract
The success of many drug design projects is fundamentally limited by the nature of the target — the target’s “druggability”. Here we define “druggability” as the ability of a target to be modulated by potent, small “drug-like” molecules (which are often suitable for oral delivery). The physico-chemical properties of “drug-like” molecules are discussed below. In turn, the “druggability” of a target can be assessed from analysis of all the available sequence, structural and ligand information coupled with an understanding the structural and thermodynamic basis of protein-ligand interactions. Thus, early target assessment can be a powerful tool for portfolio management, directing resources towards “druggable” targets, which are more likely to deliver clinical candidates.
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Hopkins, A.L., Groom, C.R. (2003). Target Analysis: A Priori Assessment of Druggability. In: Waldmann, H., Koppitz, M. (eds) Small Molecule — Protein Interactions. Ernst Schering Research Foundation Workshop, vol 42. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-05314-0_2
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DOI: https://doi.org/10.1007/978-3-662-05314-0_2
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