Table 1.
SARs of Compounds with Various Covalent Warheads
| |||
|---|---|---|---|
|
| |||
| Compound | X | R | G9a adduct (%)a |
|
| |||
| 1 | N |
|
40% |
| 2 | N |
|
ND |
| 3 | N |
|
ND |
| 4 | N |
|
ND |
| 5 | N |
|
ND |
| 6 | N |
|
ND |
| 7 | N |
|
ND |
| 8 (MS8511) | C |
|
50% |
Formation of G9a adduct was monitored by mass spectrometry. G9a adduct (%) = (G9a adduct/(G9a + G9a adduct)) × 100.
ND: G9a adduct was not detected.