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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 5. Carboline analogues from Boehringer-Ingelheim Pharmaceuticals.

graphic file with name nihms-735690-t0053.jpg

Compd R1 R1, R2 IC50a (nM) EC50b (nM)
33 NH2 5400
34 graphic file with name nihms-735690-t0054.jpg 520
35 graphic file with name nihms-735690-t0055.jpg 820
36 graphic file with name nihms-735690-t0056.jpg 89
37 graphic file with name nihms-735690-t0057.jpg 72
38 graphic file with name nihms-735690-t0058.jpg 34
39 graphic file with name nihms-735690-t0059.jpg 44 1600
40 graphic file with name nihms-735690-t0060.jpg 10 >5000
41 graphic file with name nihms-735690-t0061.jpg 20 1400
42 graphic file with name nihms-735690-t0062.jpg 5 >5000
43 graphic file with name nihms-735690-t0063.jpg H, Me 7 8900
44 graphic file with name nihms-735690-t0064.jpg H, Me 4 1670
45 graphic file with name nihms-735690-t0065.jpg H, Me 3 735
46 graphic file with name nihms-735690-t0066.jpg Me, Me 2 430
47 graphic file with name nihms-735690-t0067.jpg -(CH2)3- 2 300
a

Expressed as the inhibition of MK2 in a DELFI assay.

b

Expressed as the ability to inhibit TNFα production in LPS-stimulated THP-1 cells.