Table 1.
R1 | R2 | FLuc IC50, μM | FLucUGA EC50, μM | FLucUGA % activation | ||
o-F | m-COOH | (1) | 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.