Table 2. Optimization of the Bisamide Solubilizing Group.

^apGI₅₀ = −log GI₅₀ (M); geometric mean ± SEM, n = number of biological repeats in parentheses. For the corresponding SK-OV-3 HSP72 cell-based ELISA data See Supporting Information.

^bMouse liver microsome (MLM) assay was carried out at Cyprotex, arithmetic mean of n = 2. In vitro Cl_int is calculated from the half-life using standard procedures and assumes the fraction unbound in the assay is 1.³⁷

^cKinetic solubility (KS) measured via an in-house HPLC method from phosphate buffer at pH 7.4, all values quoted to 1 SF, the dynamic range of the assay is 1–100 μM, arithmetic mean of n = 2.

^dMeasured via an in-house HPLC method, arithmetic mean of n = 2, all values quoted to 2 SF.³⁸

^eMoKa version 2.5.2, all values quoted to 2 SF. See Supporting Information for details.