Table 4. Distal Core SAR Exploration^a.

^aAll assay results are reported as the geometric mean of at least two separate runs.

^bPI3Kδ activities were measured with an ATP concentration fixed at the K_m of PI3Kδ by HTRF, where the PIP3 product is detected by displacement of biotin-PIP3 from an energy transfer complex.

^cTHP-1 cells were treated with compounds for 30 min, stimulated with M-CSF at EC₈₀ for 3 min and then lysed to measure (by ELISA) pAkt (Thr308) produced through PI3Kδ.

^dPercent metabolism expressed as disappearance of parent compound after microsomal incubation for 30 min (1 mg/mL protein and 5 μM compound at 37 °C).