Table 2. Pyrrolopyridinone derivatives from Pfizer.
| |||
---|---|---|---|
Compd | R | IC50a (nM) | EC50b (nM) |
3 | H | 171 | 19000 |
4 | Ph | 66 | 1400 |
5 | 2-F-Ph | 126 | 4800 |
6 | 3-naphthyl | 52 | 4200 |
7 | 3-quinoline | 8.5 | 4400 |
Expressed as the inhibition of MK2 ability to phosphorylate the KKKALSRQLSVAA peptide.
Expressed as the ability to inhibit TNFα production in LPS-stimulated U937 cells.