Figure 6.
Binding of selected macrocycles to EPHA2 and GAK measured by SPR. (A) Affinity fits for compounds 6 (KD (EPHA2) = 307.0 ± 5.4; KD (GAK) = 112.4), 23 (KD (EPHA2) = 120.4 ± 6.5; KD (GAK) = 7.7), 28 (KD (EPHA2) = NA; KD (GAK) = 49.7), and 55 (KD (EPHA2) = 180.5 ± 5.0; KD (GAK) = 19.2) determined by SPR . (B): Sensorgram for compounds 23, 28, and 55 for EPHA2 and GAK with kinetic-fit KD values. SPR experiments were conducted in duplicates for EPHA2 and as a single measurement for GAK (five point dose response).
