Table 5. Carboline analogues from Boehringer-Ingelheim Pharmaceuticals.
| ||||
---|---|---|---|---|
Compd | R1 | R1, R2 | IC50a (nM) | EC50b (nM) |
33 | NH2 | 5400 | ||
34 | 520 | |||
35 | 820 | |||
36 | 89 | |||
37 | 72 | |||
38 | 34 | |||
39 | 44 | 1600 | ||
40 | 10 | >5000 | ||
41 | 20 | 1400 | ||
42 | 5 | >5000 | ||
43 | H, Me | 7 | 8900 | |
44 | H, Me | 4 | 1670 | |
45 | H, Me | 3 | 735 | |
46 | Me, Me | 2 | 430 | |
47 | -(CH2)3- | 2 | 300 |
Expressed as the inhibition of MK2 in a DELFI assay.
Expressed as the ability to inhibit TNFα production in LPS-stimulated THP-1 cells.