Table 10. SAR for thienopyrimidine series for Nek4.
| |||||
Compound | R 1 | R 2 | Nek4 IC50 nM | Nek4 % Inh | COT IC50 (nM) |
Abbott Cmpd 17 | 50 | — | 1120 | ||
Genentech Cmpd 1 | — | 47.5 a | 410 | ||
Genentech Cmpd 2 | — | 89.9 a | 150 | ||
Genentech Cmpd 32 | — | 8.7 b | — | ||
Abbott Cmpd 3359 | 316 | — | — | ||
Abbott Cmpd 3357 | 1000 | — | — |
a100 nM screening concentration.
b1 μM screening concentration.