Table 1. CRE-LUC Activity and ADME Properties of Fused 3-Hydroxy-3-trifluoromethylpyrazole Derivatives.

^aCellular assay. EC₅₀ values represent arithmetic means of n reported determinations. These assay generally produced results within 2-fold of the reported mean. Compound 1 (Y-27632) was used as a standard and positive control for the assay.

^bFold increase is considered as the measure of the difference of maximum efficacy calculated from the concentration response curve fit of the normalized CRE-LUC activity of the mutant Htt expressing cells (E_max-ind) and of the noninduced cells (E_max-nonind).

^cPermeability assay A:B (10^–6 cm/s).

^dEfflux ratio measured in MDCK-MDR1 permeability assay (B:A/A:B).

^eKinetic solubility.