Abstract: In certain embodiments, this invention pertains to the creation of “Sparse Matrix” libraries of compounds. The sparse matrix libraries of this invention typically span an n-dimensional parameter (property) space at extremely sparse intervals and thereby provide a relatively small library of compounds (e.g., a library of about 200 or fewer compounds) that can be used to quickly and efficiently screen the compound parameter space for one or more desired physical, chemical, or biological properties (e.g., binding specificity, binding avidity, ?toxicity, solubility, mobility, cell permeability, serum half-life, biocompatibility, etc.).