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. Author manuscript; available in PMC: 2014 Mar 19.
Published in final edited form as: ACS Chem Biol. 2012 Jan 19;7(3):526–534. doi: 10.1021/cb200439z

Table 1.

Comparison of results of our FP competitive binding assay to reported anti-influenza activities of known endonuclease inhibitors. Reported FP values are the average of triplicate measurements ± standard error of the mean (SEM). ND = no data.

Compound Structure Reported IC50 (MM) FP EC50 (MM) FP Ki (MM) BEIa LEIb
1 (DPBA) graphic file with name nihms-553146-t0004.jpg R = H 21.3c 2.07 ± 0.03 0.48 ± 0.01 33.0 0.62
5 R = Ph 3.7c 3.56 ± 0.07 0.96 ± 0.02 22.5 0.42
6 R = piperazine ND 1.5 ± 0.8 0.3 ± 0.3 23.7 0.45
7 R = methoxy ND 6.7 ± 0.1 1.97 ± 0.03 25.7 0.49
8 R = oxyphenyl ND 1.45 ± 0.07 0.28 ± 0.02 23.1 0.43
9 R = benzyloxy ND 6.8 ± 0.2 1.99 ± 0.06 19.1 0.30
2 (L-742,001) graphic file with name nihms-553146-t0005.jpg R = Ph 0.430c 0.86 ± 0.04 0.09 ± 0.01 17.0 0.34
10 R = cyclohexane 0.33c 0.8 ± 0.2 0.084 ± 0.001 16.9 0.34
3 graphic file with name nihms-553146-t0006.jpg 15.0d 3.22 ± 0.04 0.85 ± 0.02 34.3 0.65
11 graphic file with name nihms-553146-t0007.jpg ND 6.8 ± 0.5 2.0 ± 0.2 27.8 0.52
12 graphic file with name nihms-553146-t0008.jpg ND 8.17 ± 0.02 2.440 ± 0.006 24.0 0.46
13 graphic file with name nihms-553146-t0009.jpg ND >250
14 graphic file with name nihms-553146-t0010.jpg ND >250
15 graphic file with name nihms-553146-t0011.jpg ND >250
16 graphic file with name nihms-553146-t0012.jpg R = CH3 >500c >250
17 R = tert-butyl ND >250
18 graphic file with name nihms-553146-t0013.jpg >500c >250
19 graphic file with name nihms-553146-t0014.jpg >500c >250
a

BEI = Binding efficiency index based on FP data (pKi,/MW), where MW is molecular weight in kDa (55).

b

LE = Ligand efficiency based on FP data (ΔG/N), where ΔG = -RTlnKi and N is the number of heavy atoms (56).

c

Published results in an influenza virus in vitro transcription assay (29).

d

Published results in an influenza virus in vitro transcription assay (53).