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. 2010 Mar 1;107(11):4878–4883. doi: 10.1073/pnas.0909141107

Table 1.

Potency and cellular activity of analogs in the enzymatic (FLuc) and cell-based (FLucUGA) assays

R1 R2 FLuc IC50, μM FLucUGA EC50, μM FLucUGA % activation
o-F m-COOH (1) graphic file with name pnas.0909141107figX1.jpg 0.014 ± 0.008 0.11 ± 0.09 1345 ± 391
o-F H (2) 0.99 ± 0.59 11.9 ± 5.8 812 ± 268
o-F m-CONH2 (3) 4.6 ± 1.9* 4.3 ± 2.9 1019 ± 262
o-F m-tetrazole (4) 2.9 ± 1.7 10.2 ± 5.2 618 ± 59
m-Cl m-COOH (5) 0.023 ± 0.01 0.25 ± 0.23 1013 ± 319
o-F m-CO(AMP) (6) 0.020 ± 0.01 N/A N/A
o-F p-COOH (7) 0.72 ± 0.45 3.1 ± 4.9 1288 ± 510
o-F p-CONH2 (8) 4.3 ± 2.0* 0.77 ± 0.05 1816 ± 982
o-F p-tetrazole (9) 14.5 ± 5.0 16.5 ± 3.0 528 ± 189
o-F o-COOH (10) 11.7 ± 3.2* 23.0 ± 10.8 369 ± 209
o-F o-CONH2 (11) 18.9 ± 7.6* 8.2 ± 9.7 118 ± 92
o-F m-CONH(sa-Ade) (12) 0.005 ± 0.001 N/A N/A
o-F p-CONH(sa-Ade) (13) 0.003 ± 0.001 N/A N/A

N/A, not applicable; sa-Ade, acylsulfamide adenosine; error is SD from replicates performed on different days for enzyme (n = 3) and cell-based (n = 2) assays.

*Equals partial inhibition of FLuc observed, e.g., % inhibition (x) was 40% < x ≤ 80%. See SI Text for additional details.