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. Author manuscript; available in PMC: 2016 Jul 15.
Published in final edited form as: Eur J Med Chem. 2015 May 27;100:197–209. doi: 10.1016/j.ejmech.2015.05.042

Table 1.

rPR, rKcat/KM, and IC50 values of 1–4, 16–22, and 28–30

Compd rPRa (%) Km (μM) kcat (s−1) rkcat/Km (%) IC50 (μM)
1 100 2.4 ± 0.7 8.6 100 2.0 ± 0.3
2 40.0 ± 11.2 24.3 ± 2.1 5.1 5.8 37.5 ± 6.3
3 78.7 ± 3.4 7.5 ± 3.2 5.9 21.6 13.5 ± 2.1
4 79.4 ± 7.8 10.7 ± 1.2 6.1 15.7 8.9 ±2.2
16 35.2 ± 5.3 nd nd nd nd
17 24.5 ± 7.8 nd nd nd nd
18 44.4 ± 8.7 nd nd nd nd
19 18.8 ± 4.8 nd nd nd nd
20 19.5 ± 5.3 nd nd nd nd
21 45.2 ± 3.8 80.1 ± 37.6 5.9 2.0 >250
22 38.0 ± 6.5 39.8 ± 10.4 5.4 3.7 >250
28 19.2 ± 4.5 nd nd nd nd
29 14.5 ± 4.8 nd nd nd nd
30 12.3 ± 8.7 nd nd nd nd
a

rPr: Phosphorylation rate relative to that of dThd. SDs are based on at least three measurements. nd: not determined. The following compound concentrations were used: rPR values: 100 μM nucleoside analogue and 100 μM ATP; Km and kcat values: 1.95–500 μM nucleoside analogue and 100 μM ATP; IC50 values: 0.5 μM dThd, 5 mM ATP, and 0–250.00 μM nucleoside analogue.