Table 1. Impact of 3-Indole Substitution on Potency^a.

^aRelative % bound at 10 μM of compound at 0.02, 0.2, 2, and 20 h.

^bObserved rate (k_obs/[I] M^–1 s^–1) derived from 0.02, 0.2, 2, and 20 h of relative % bound at 10 μM compound.

^cDose response GDP-KRAS^G12C/C118A (1–169) SOS1-catalyzed GTP exchange assay.

^dQuantification of phospho-ERK1/2 following compound treatment and EGF stimulation by MSD assay in MIA PaCa-2 cells. For number of replicates, mean, and standard deviations, see the Supporting Information.