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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 3. β-Carboline derivatives from Pfizer.

graphic file with name nihms-735690-t0047.jpg
Compd R R1 X IC50a (nM)
8 6-OMe 1-COOH NH 2500
9 6-OH 1-COOH NH 4500
10 6-COOMe 1-COOH NH 6600
11 6-OMe 1-COOH NMe 1000
12 6-OMe 1-COOH NEt 5800
13 6-OMe 1-COOH, 4-Me NH 2200
14 6-OMe 1-COOH, 4-Et NH 2200
15 6-OMe 1-COOH, 3-CH2OH NH 3000
16 6-OMe 1-COOH, 3-CH2NH NH 5900
17 H CH2 290
18 H CH2CH2 5100
19 n-Pr CH2 10100
a

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