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