Scheme 1. Structural Formulas of the Three Compounds Used in This Work.
Affinities for p53-Y220C core domain as measured by (direct) ITC are KD (PK5174) = 15.5 μM and KD (PK5176) = 20.6 μM.14 The affinity of PK5211 (3) was determined indirectly as KD (PK5211) = 271 μM by competition ITC with PK5174 (1); see also Figure 2.