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. Author manuscript; available in PMC: 2020 Feb 1.
Published in final edited form as: Chembiochem. 2018 Dec 27;20(3):394–407. doi: 10.1002/cbic.201800593

Table 1.

Exploration of pyrrolidin-2-one ring substitutions in the 1 scaffold.

graphic file with name nihms-1019449-t0037.jpg
compd R1 IC50 ± SD
[μM]a 		Hill coeff b % Activity
ESIc
1 graphic file with name nihms-1019449-t0038.jpg 4.0 ± 0.2 2.34 ± 0.19 1.40 ± 0.1
1a graphic file with name nihms-1019449-t0039.jpg 17.1 ± 1.2 2.57 ± 0.40 6.04 ± 0.46
1b graphic file with name nihms-1019449-t0040.jpg 3.6 ± 0.6 1.65 ± 0.38 61.74 ± 4.31
1c graphic file with name nihms-1019449-t0041.jpg 47.2 ± 8.4 1.46 ± 0.26 9.01 ± 0.78
1d graphic file with name nihms-1019449-t0042.jpg 48.5 ± 3.8 2.89 ± 0.32 14.64 ± 0.74
1e graphic file with name nihms-1019449-t0043.jpg 8.5 ± 0.7 2.93 ± 0.48 3.09 ± 0.25
1f graphic file with name nihms-1019449-t0044.jpg 10.7 ± 2.5 1.48 ± 0.13 59.42 ± 1.61
a

All experiments to determine IC50 values were run with at least duplicates at each compound dilution, IC50 values were averaged when determined in two or more independent experiments.

b

Hill coefficient obtained upon fitting the concentration-response curves.

c

DGC activity of the enzyme-substrate-inhibitor complex.