Table 1. IC50 Values (in nM) Calculated for PP1, 7i–k, 8d, 9d, 11a, and Dasatinib in a Selection of Recombinant Kinases.
kinase \ hit | PP1 | 7i | 7j | 7k | 8d | 9d | 11a | dasatinib |
---|---|---|---|---|---|---|---|---|
ABL | 147 | 6323 | 7525 | 7249 | 1207 | 116 | 479 | <0.5 |
FYNa | 27 | 311 | 913 | 1964 | 1226 | 38 | 2.1 | <0.5 |
KIT | 1318 | >104 | >104 | >104 | >104 | >104 | >104 | 39 |
mTOR | 9318 | >104 | >104 | >104 | 328 | 8565 | >104 | >104 |
PDGFRα | 657 | >104 | >104 | >104 | >104 | >104 | >104 | 9.9 |
RET | 11 | 6584 | >104 | >104 | 598 | 289 | >104 | 433 |
SRCa | 17 | 126 | 303 | 1040 | 2453 | 27 | <0.5 | <0.5 |
YESa | 36 | 71 | 344 | 696 | 566 | 12 | <0.5 | <0.5 |
IC50(ABL) /IC50(SRC) | 8 | 50 | 25 | 7 | 0.5 | 4 | >950 | 1 |
Member of SFK.