Table 1.
Inhibitory effect of some non-selective JmjC inhibitors (2–6) and inhibitors that are more selective for some JmjC subfamilies (7–10)
| pIC50a KDM |
|||||||
|---|---|---|---|---|---|---|---|
| 2A | 3A | 4C | 4E | 5A | 5C | 6B | |
| 2 14 | 4.3 | 5.7 | <4.0 | 5.1 | 6.5 | ||
| 3 14 | 5.4 | 5.1 | 5.6 | 5.2–6.0 | 6.3 | 4.5 | |
| 4 15 | 5.3 | 6.0 | 5.5 | 5.3 | 7.5 | 5.0 | |
| 5 14 | 4.8 | 6.8 | 6.2 | 6.5 | 4.6 | 7.0 | |
| 6 16 | 6.0 | 6.5 | 6.6 | 6.1 | |||
| 7 17 | 5.5 | 5.2 | 4.4 | ||||
| 8 18,19 | 4.4 | 4.7 | 7.2 | ||||
| 9 20 | 5.2 | 4.1 | 4.3 | ||||
| 10 21 | 5.8 | <4.0 | <4.0 | <4.0 | <4.0 | ||
a
Reported values determined in amplified luminescent proximity homogeneous assay (AlphaScreen), enzyme-linked immunosorbent assay (ELISA), dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) or matrix-assisted laser desorption/ionization (MALDI) assay.