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

Table 2.

Variation of the bicyclic scaffold.

Compound graphic file with name fx11.gif Kd ± SDa (µM) IC50 ± SDb (µM)
9 graphic file with name fx12.gif 1.5 ± 1 1.3 ± 0.2



13 graphic file with name fx13.gif >100 nd



14 graphic file with name fx14.gif 21 ± 4.2 >100



15 graphic file with name fx15.gif >100 nd



16 graphic file with name fx16.gif 1.6 ± 0.1 5.3 ± 0.8



17 graphic file with name fx17.gif 1.3 ± 0.1 3.8 ± 0.3



18 graphic file with name fx18.gif >100 nd



19 graphic file with name fx19.gif 10.0 ± 1.4 10.4 ± 0.2

X, R = Me; Y, R = 3-pyrolidine;

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.