Table 8. Pyrrolopyrimidinones and pyrazoles from Novartis.
| |||
---|---|---|---|
Compd | R | IC50a (nM) | EC50b (nM) |
60 | F | 200 | 350 |
61 | 51 | 110 | |
62 | 2000 | ||
63 | p-OMe | 84 | |
64c | 82 | 5300 (4100) | |
65c | 61 | 2500 (2000) |
Expressed as the inhibition of MK2 activity toward a peptide substrate.
Expressed as the ability to inhibit TNFα production in hPBMC cells stimulated with both LPS and IFNγ, and to inhibit Hsp27 phosphorylation in anisomycin-stimulated THP-1 cells (in parentheses).
R group is in meta position.