Characteristic functional annotations allow one to catalog or compare observable differences in kinetic response to various in vitro simuli of an enzyme's active site. These variants potentially span the continuum of kinetic sub-states acquired by natural gating mechanisms, allosteric factors, post-translational modifications, family and mutation amino-acid sequence, or splice variants. ProFACT's Conformerics™ plaform encompasses methods to compartmentalize functional variants, methods to challenge these variants with small molecules, and strategies to evaluate drug response and mechanism of action from natural sources.