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. Author manuscript; available in PMC: 2015 Mar 15.
Published in final edited form as: Bioorg Med Chem Lett. 2014 Feb 7;24(6):1538–1544. doi: 10.1016/j.bmcl.2014.01.079

Table 1.

Activity data for tag-free photoprobes 10, 19, and 27.

graphic file with name nihms568292u1.jpg
Cmpd R1 R2 T/C (5 μM)a Growth T/C (50 μM)b IC50 (μM)c
10a propargyl 8-Bz 0.77 ± 0.34 1.09 ± 0.04 nd
10b graphic file with name nihms568292t1.jpg 8-Bz 0.51 ± 0.07 0.94 ± 0.18 3.8 ± 0.6
19a propargyl graphic file with name nihms568292t2.jpg 1.07 ± 0.16 0.96 ± 0.09 nd
19b graphic file with name nihms568292t3.jpg graphic file with name nihms568292t4.jpg 0.49 ± 0.34 1.07 ± 0.02 0.33 ± 0.70
19c graphic file with name nihms568292t5.jpg graphic file with name nihms568292t6.jpg 0.71 ± 0.40 1.01 ± 0.09 nd
19d graphic file with name nihms568292t7.jpg 8-O-propargyl 0.89 ± 0.16 1.02 ± 0.01 nd
27 graphic file with name nihms568292t8.jpg 9-N3 0.30 ± 0.08 0.98 ± 0.04 0.19 ± 0.26
4 Et 9-OMe 0.10 ± 0.06 0.73 ± 0.07 1.3 ± 0.6
a

Amount of SK activity in GAS culture measured via colorimetric assay (A405) after incubation with 5 μM test compound for 24 hours divided by SK activity measured in GAS culture 24 hours after treatment with DMSO control, +/− standard deviation.

b

Growth inhibition as measured by OD600 of GAS culture 24 hours after treatment with 50 μM test compound divided by OD600 of control GAS culture treated with DMSO control after 24 hours, +/− standard deviation.

c

Concentration at which 50% maximal inhibitory effect against SK expression was achieved +/− standard deviation. Each data point is derived from the statistical treatment of at least 3 replicates. nd = not determined.