ID: ALA3887468
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.
Bioactivity
Activity Types for Assay ALA3887468
IC50
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 |
586.78 | 4.35 | 4.35 |
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 |
385.51 | 3.09 | 3.09 |
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 |