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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 4. Polycondensed benzothiophene derivatives from Pfizer.

graphic file with name nihms-735690-t0048.jpg
Compd R1 R2 IC50a (nM) EC50b (nM)
20 H H 180 1400
21 Me H 40 700
22 H Me 300 3800
23 CH2OH H 14 400
24 CH2NH H 5 2600
25 16 90
26 H 1 50
27 Cl 2 130
28 Ph 9 180
29 graphic file with name nihms-735690-t0049.jpg 5 220
30, PF022 graphic file with name nihms-735690-t0050.jpg 5 150
31, PF318 graphic file with name nihms-735690-t0051.jpg 25 255
32, PF029 graphic file with name nihms-735690-t0052.jpg 2 150
a

Expressed as the inhibition of MK2 ability to phosphorylate the KKKALSRQLSVAA peptide.

b

Expressed as the ability to inhibit TNFα production in LPS-stimulated U937 cells.