Table 1.
Binding affinities (Ki, nM) for PKCα and RasGRP3 for compounds 12a-l.
 | |||||||
|---|---|---|---|---|---|---|---|
| R1 | R2 | SLog P | PKCα Ki (nM) | PKCα Z/E (Ki) | RasGRP3 Ki (nM) | RasGRP3 Z/E (Ki) | |
| 12a-E |
|
|
2.0660 | 1020 ± 100 | — | 23.8 ± 2.6 | — |
| 12b-E |
|
|
2.0660 | 790 ± 100 | 43 | 59 ± 13 | 33 |
| 12b-Z |
|
|
2.0660 | 34100 ± 3300 | 1970 ± 360 | ||
| 12c-E |
|
|
2.0660 | 1110 ± 200 | 30 | 54± 13 | 44 |
| 12c-Z |
|
|
2.0660 | 33200 ± 4300 | 2360 ± 150 | ||
| 12d-E |
|
|
3.2192 | 150 ± 21 | 105 | 11.0 ± 1.9 | 185 |
| 12d-Z |
|
|
3.2192 | 15800 ± 5400 | 2040 ± 400 | ||
| 12e-E |
|
|
3.2192 | 755 ± 75 | 6.5 | 137 ± 16 | 10 |
| 12e-Z |
|
|
3.2192 | 4880 ± 640 | 1410 ± 130 | ||
| 12f-E |
|
|
3.2192 | 174 ± 18 | — | 3.7 ± 0.8 | — |
| 12g-E |
|
|
2.0086 | 1130 ± 390 | 24 | 35.8 ± 4.8 | 69 |
| 12g-Z |
|
|
2.0086 | 27100 ± 3000 | 2470 ± 360 | ||
| 12h-E |
|
|
2.0086 | 810 ± 130 | 26 | 81 ± 12 | 68 |
| 12h-Z |
|
|
2.0086 | 21200 ± 5600 | 5500 ±1200 | ||
| 12i-E |
|
|
2.0086 | 1450 ± 150 | 18 | 54.2 ± 7.2 | 68 |
| 12i-Z |
|
|
2.0086 | 25400 ± 1700 | 3660 ± 750 | ||
| 12j-E |
|
|
3.1618 | 132 ± 8.6 | 22 | 8.2 ± 1.1 | 170 |
| 12j-Z |
|
|
3.1618 | 2940 ± 260 | 1390 ± 130 | ||
| 12k-E |
|
|
3.1618 | 144 ± 20 | 35 | 17.4 ± 1.7 | 52 |
| 12k-Z |
|
|
3.1618 | 5100± 550 | 907 ± 98 | ||
| 12l-E |
|
|
3.4645 | 212 ± 35 | — | 3.3 ± 1.5 | — |