Skip to main content
. 2019 Apr 15;29(8):1023–1029. doi: 10.1016/j.bmcl.2019.01.035

Table 4.

Further substitutions of the pyrazolopyridinone scaffold.

Compound R1-group
 R2-group
 Kd ± SDa (µM) IC50 ± SDb (µM)
graphic file with name fx26.gif
25 N H >500 nd
2 N graphic file with name fx27.gif 29.5 ± 8.3 67.6 ± 2.4
26 graphic file with name fx28.gif graphic file with name fx29.gif 0.60 ± 0.05 0.63 ± 0.15
27 graphic file with name fx30.gif graphic file with name fx31.gif 0.27 ± 0.04 0.33 ± 0.06
28 graphic file with name fx32.gif graphic file with name fx33.gif 0.09 ± 0.02 0.24 ± 0.01
a

Kd: SPR binding affinity, values are mean ± standard deviation from n = 2–10 separate experiments.

b

IC50: compound concentration that reduces actin bundling by 50%, values are mean ± standard deviation from n = 2–4 separate experiments; nd: not determined.