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. Author manuscript; available in PMC: 2017 Apr 28.
Published in final edited form as: J Med Chem. 2015 Nov 9;59(8):3609–3634. doi: 10.1021/acs.jmedchem.5b01457

Table 8. Pyrrolopyrimidinones and pyrazoles from Novartis.

graphic file with name nihms-735690-t0083.jpg
Compd R IC50a (nM) EC50b (nM)
60 F 200 350
61 graphic file with name nihms-735690-t0084.jpg 51 110
62 2000
63 p-OMe 84
64c graphic file with name nihms-735690-t0085.jpg 82 5300 (4100)
65c graphic file with name nihms-735690-t0086.jpg 61 2500 (2000)
a

Expressed as the inhibition of MK2 activity toward a peptide substrate.

b

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).

c

R group is in meta position.