Table 7.
Efficacy of compounds containing novel methyl-lysine mimicsa
| ID | R | LANCE IC50 (μM) | AlphaScreen IC50 (μM) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| L3MBTL3 | L3MBTL3 | L3MBTL1 | L3MBTL4 | SFMBT1 | MBTD1 | CBX7 | 53BP1 | UHRF1 | PHF23 | JARID1A | ||
| 53 |
|
0.35 ± 0.15 (4) | 0.37 ± 0.053 (3) | 4.0 ± 1.3 (3) | >10 (3) | >10 (5) | >10 (10) | >10 (4) | >10 (8) | >10 (3) | >10 (3) | >10 (3) |
| 54 |
|
0.15 ± 0.059 (4) | 0.24 ± 0.0058 (3) | 6.8 ± 2.4 (3) | >10 (3) | >10 (5) | >10b (11) | >10 (4) | >10b (10) | >10 (3) | >10 (3) | >10 (3) |
| 2 |
|
0.16 ± 0.075 (4) | 0.17 ± 0.010 (3) | >10b (3) | >10 (3) | >10 (5) | >10b (10) | >10 (4) | >10 (9) | >10 (3) | >10 (3) | >10 (3) |
| 55 |
|
0.16 ± 0.035 (4) | 0.17 ± 0.023 (3) | 6.6 ± 2.0 (3) | >10 (3) | >10 (5) | 3.5 ± 1.1b (11) | >10 (4) | 3.5 ± 1.1b (10) | >10 (3) | >10 (3) | >10 (3) |
| 56 |
|
0.14 ± 0.045 (4) | 0.13 ± 0.025 (3) | 9.6 ± 1.2b (3) | >10 (3) | >10 (5) | 5.1 ± 1.1b (11) | >10 (4) | >10b (10) | >10 (3) | >10 (3) | >10 (3) |
a
The data for the average IC50 values was calculated from the number of replicate runs indicated in parentheses.
b
IC50 values were calculated by averaging data points for each compound concentration and plotted using 4-parameter curve fitting when IC50 values for a single compound were not all active (< 10 μM) or inactive (> 10 μM).