Table 2.
Molecule | IC50 (μM) | Ki (μM) | Phosphohydrolase specific activity (Percentage of GTP)a | Inhibitory potentialb |
---|---|---|---|---|
GTP | 87 | 16 | 100 | 1.0 |
dGTP | 76 | 14 | 99 | 1.1 |
A-3 | 83 | 15 | 88 | 1.2 |
A-4 | 8.1 | 1.5 | 18 | 60 |
A-5 | 150 | 27 | 17 | 3.4 |
A-6 | 53 | 9.6 | 70 | 2.4 |
A-8 | 10 | 1.8 | 10 | 86 |
A-9 | 16 | 2.9 | 41 | 13 |
A-10 | 93 | 17 | 20 | 4.7 |
A-11 | 2.0 | 0.4 | 16 | 268 |
A-12 | 6.1 | 1.1 | 138 | 10 |
A-13 | 32 | 5.9 | 109 | 2.5 |
A-15 | 49 | 8.8 | 111 | 1.6 |
A-17 | 59 | 11 | 116 | 1.3 |
A-18 | 8.1 | 1.5 | 12 | 89 |
A-19 | 61 | 11 | 38 | 3.8 |
A-20 | 2.0 | 0.4 | 7.2 | 597 |
A-22 | 113 | 21 | 81 | 0.9 |
A-24 | 8.1 | 1.5 | 7.2 | 149 |
Tripoly-PO4 | 0.4 | 0.1 | 3.6 | 5965 |
aThe phosphohydrolase specific activities were calculated from the slopes of the titration curves and normalized to the specific activity for the hydrolysis of GTP.
bThe inhibitory potential is defined by the following equation:
(KiGTP/KiMolecule) × (Spec. activityGTP/Spec. activityMolecule)