TABLE 1.
IC50 (μM) |
||||||
---|---|---|---|---|---|---|
structure | Original target(s) | β-Lactamase | Chymotrypsin | cDHFR | β-Gal | |
0.5 β-Lactamaseb | 0.5 | 2.5 | 5 | 15 | ||
5 β-Lactamaseb | 5 | 25 | 35 | 90 | ||
5 β-Lactamaseb | 5 | 15 | N.D. | N.D. | ||
8 Malarial protease | 10 | 55 | 70 | 180 | ||
7 pDHFR | 10 | 50 | 60 | 300 | ||
80 pDHFR | 50 | 25 | N.D. | 600 | ||
50 HIV Tar RNA | 10 | 90 | N.D. | 600 | ||
3 TS | 30 Kinesin | 3 | 11 | 20 | 200 | |
20cInsulin receptor | 7.5 Kinesin | 16 | 50 | N.D. | 80 | |
5.2 VEGF | 10.0 IGF-1 | 6 | 30 | 30 | 55 | |
25 Farnesyltransferase | 3 | 9 | 25 | 150 | ||
15dGyrase | 18 | 100 | 150 | 320 | ||
1 Prion | 30.4 TIM | 3.9 | 40 | 0.4 | 100 | |
17 eNOS | 24 nNOS | 7 | 60 | N.D. | N.D. | |
3.8 PI3K | 11.0 Integrase | 4 | 100 | N.D. | 220 |
Abbreviations: cDHFR, chicken DHFR; β-gal, β-galactosidase; pDHFR, Pneumocystis carinii DHFR; TS, thymidylate synthase; VEGF, vascular endothelial growth factor receptor tyrosine kinase; IGF-1, insulin-like growth factor receptor tyrosine kinase; TIM, triosephosphate isomerase; eNOS, endothelial nitric oxide synthase; nNOS, neuronal nitric oxide synthase; PI3K, phosphoinositide 3-kinase; N.D., not determined.
Table adapted, with permission, from Ref. [8].
Unpublished observations.
Kd.
Maximal non-effective concentration.