Table 1. Thermal Stabilization (ΔT_m) and Binding Affinities of Subsite 3 Targeting Analogues against p53-Y220C, Determined by DSF and ITC, Respectively (Previously Reported Analogues 4 and 77 Included as Positive Controls).

^aMeasured by DSF using 8 μM protein and 10× SYPRO Orange. ΔT_m values were calculated as the average of at least three independent measurements.

^bMeasured by ITC ([prot] = 50 μM). K_d values were calculated as the average of at least three independent measurements.

^cConsistent with literature values ΔT_m = 1.8 °C ([L] = 250 μM), K_d = 21 μM.⁴⁴

^dAverage of two repeats.

^eTested as a 90% pure mixture with monoiodinated analogue. K_d not recorded for mixture.

^fLiterature value.⁴² Abbreviations: SD, standard deviation; LE, ligand efficiency; NHA, number of heavy (non-hydrogen) atoms.