Table 1.
Inhibition of biotinylated fibronectin binding to α5β1 integrin compared with inhibition of biotinylated vitronectin binding to αvβ3.
| Compound | IC 50 [nM][a] α5β1 | IC 50 [nM][b] αvβ3 | IC 50 [α5β1]/IC 50 (αvβ3) |
|---|---|---|---|
| 2 | 1647±871 | 3.2±2.7 | 515 |
| 3 | 532±35 | 4.5±1.1 | 118 |
| 4 | 314±1.4 | 7.6±4.3 | 41 |
| 5 | 1217±157 | 12.2±5.0 | 100 |
| 6 | 73.3±3.7 | 2.1±0.6 | 35 |
| 7 | 25.7±6.2 | 0.2±0.09 | 128 |
| 1 a | 14.4±3.1 | 0.6±0.1 | 24 |
| 1 b | 166±28 | 3.2±1.3 | 52 |
[a] IC 50 values were calculated as the concentration of compound required for 50 % inhibition of biotinylated fibronectin binding as estimated by GraphPad Prism software; all values are the arithmetic mean±SD of triplicate determinations. [b] Calculated as the concentration of compound required for 50 % inhibition of biotinylated vitronectin binding. See Ref. 7a for 1 a and Ref. 8c for 1 b and 2–7.