Table 1.
Kinase activities on RET, VEGFR2, and RETV804M.
| Compd. | RET | VEGFR2 | RETV804M |
|---|---|---|---|
| 1 | 28% ± 3% [b], 63% ± 5%[c] | 59% ± 3%[c] | / |
| 1a | 18.2 ± 0.8 μM[a] | 89% ± 4%[c] | / |
| 2 | 2.1 ± 0.2 μM[a] | 93% ± 2%[c] | / |
| 3 | 0.006 μM[d] | 0.018 μM[d] | 0.006 μM[d] |
| 3b | 0.047 ± 0.007 μM[a] | 97% ± 2%[c] | / |
| Pz-1 (4) | < 0.001 μM[a] | < 0.001 μM[a] | < 0.001 μM[a] |
[a]
IC50 values were determined using a microfluidics separation based assay. The data were means from at least three independent experiments. [ATP] = 190 μM.
[b]
Residual activity at 100.0 μM in triplicate. [ATP] = 190 μM.
[c]
Residual activity at 20.0 μM in triplicate. [ATP] = 190 μM.
[d]
Kd values were determined using an active site-directed competition binding assay that was outsourced to KINOMEScan®.