Table 1. IC50 values of c-Fes inhibitors determined in vitro using a recombinant SH2-kinase protein and the Z′-Lyte assays.
Concentration response curves were generated using the recombinant c-Fes SH2-kinase protein and the Z′-Lyte assay as described under Experimental Procedures. Compounds are organized by chemical scaffold and predicted mode of inhibition (Type vs. Type II). See also Figure S2.
| Compound | Type (predicted) | IC50 (nM) |
|---|---|---|
| Diaminopyrimidines | ||
| TAE684 | I | 118 |
| Triaminopyrimidines | ||
| XMD5-130 | I | 308 |
| XMD6-3 | I | 275 |
| HG-5-91-01 | I | 275 |
| HG-5-145-01 | I | 537 |
| HG-5-150-01 | I | 252 |
| HG-5-56-01 | I | 654 |
| Pyrazolopyrimidines | ||
| WZ-4-49-1 | I | 214 |
| WZ-4-49-8 | I | 67 |
| WZ-4-49-9 | I | 302 |
| WZ-4-49-10 | I | 146 |
| Diaminopurines | ||
| WZ-4-24-1 | I | 168 |
| WZ-4-24-2 | I | 365 |
| WZ-4-24-3 | I | 363 |
| WZ-4-24-7 | I | 149 |
| Thiazolepyridines | ||
| HG-7-127-01 | II | 222 |
| Pyrrolopyridines | ||
| HG-7-92-01 | II | 298 |
| Pyrazines | ||
| HG-7-27-01 | II | 224 |
| Pyrimidine carbamates | ||
| WH-4-199-1 | II | 256 |
| WH-4-199-2 | II | 422 |
| WH-4-124-2 | II | 535 |