Basic Information
ID: ALA3887469
Type: Binding
Description: Inhibition Assay: Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemate Plus equipped with 384-channel head (Thermo Scientific). The final top concentration of test compounds in the assay was 10 uM. Positive control (100% inhibition standard) was 1 mM final concentration of SAH and negative control (0% inhibition standard) contained 1 uL of DMSO. Test compounds were then incubated for 30 minutes with 40 uL per well of wild-type EZH2 (final concentration was 4 nM), Y641F EZH2 (final concentration was 0.1 nM) and A677G and A687V EZH2 (for each, final concentration was 2nM) and peptide in 1x assay buffer (20 mM BICINE pH =7.6, 1 mM DTT, 0.002% TWEEN 20 (generic: polysorbate 20), 0.005% BSG). For the wild-type EZH2 and A677G EZH2 assays, biotinylated peptide H3:21-44 with unmethylated K27 was present at a final concentration of 200 nM, while in the A687V EZH2 assay, biotinylated peptide H3.
Activity Charts
Bioactivity
Activity Types for Assay ALA3887469
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 384.42 | -1.44 | -1.44 |
| 539.68 | 4.89 | 4.89 |
| 518.71 | 4.33 | 4.33 |
| 558.73 | 3.71 | 3.71 |
| 516.69 | 4.39 | 4.39 |
| 530.72 | 4.69 | 4.69 |
| 600.80 | 5.38 | 5.38 |
| 651.65 | 5.50 | 5.50 |
| 593.17 | 5.08 | 5.08 |
| 590.74 | 4.87 | 4.87 |
| 615.82 | 4.71 | 4.71 |
| 600.81 | 4.69 | 4.69 |
| 514.63 | 3.75 | 3.75 |
| 445.99 | 4.14 | 4.14 |
| 480.70 | 5.05 | 5.05 |
| 439.60 | 3.32 | 3.32 |
| 487.09 | 4.84 | 4.84 |
| 502.06 | 4.83 | 4.83 |
| 502.70 | 4.69 | 4.69 |
| 537.93 | 5.04 | 5.04 |
| 526.69 | 4.58 | 4.58 |
| 487.09 | 4.59 | 4.59 |
| 523.07 | 5.22 | 5.22 |
| 462.64 | 3.91 | 3.91 |
| 458.05 | 5.68 | 5.68 |
| 460.02 | 4.26 | 4.26 |
| 530.74 | 3.72 | 3.72 |
| 478.64 | 4.27 | 4.27 |
| 473.06 | 4.58 | 4.58 |
| 504.72 | 5.54 | 5.54 |
| 527.11 | 4.89 | 4.89 |
| 531.54 | 5.00 | 5.00 |
| 416.95 | 3.02 | 3.02 |
| 515.10 | 4.35 | 4.35 |
| 513.13 | 5.51 | 5.51 |
| 521.71 | 3.78 | 3.78 |
| 527.11 | 4.89 | 4.89 |
| 487.09 | 4.92 | 4.92 |
| 518.75 | 5.33 | 5.33 |
| 474.00 | 4.35 | 4.35 |
| 473.06 | 4.45 | 4.45 |
| 368.44 | 2.29 | 2.29 |
| 486.10 | 6.31 | 6.31 |
| 468.64 | 3.94 | 3.94 |
| 520.72 | 4.05 | 4.05 |
| 487.09 | 4.84 | 4.84 |
| 474.00 | 4.35 | 4.35 |
| 502.06 | 4.83 | 4.83 |
| 485.07 | 4.73 | 4.73 |
| 472.07 | 5.92 | 5.92 |
| 506.61 | 4.95 | 4.95 |
| 501.12 | 5.23 | 5.23 |
| 512.66 | 4.24 | 4.24 |
| 523.72 | 3.62 | 3.62 |