Table 13. Squarate derivatives from Wyeth Research.
| ||||
---|---|---|---|---|
Compd | R | R1 | R2 | IC50a (μM) |
92 | H | Me | Ph | 8.9 |
93 | H | Me | Ph | >100 |
94 | H | H | Ph | 88 |
95 | H | Me | m-OH-Ph | 0.38 |
96 | H | CONH2 | m-OH-Ph | 0.39 |
97 | Me | Ph | 0.67 |
Expressed as the inhibition of MK2 activity toward a peptide substrate.