Assay Detail
Binding
CHEMBL3887470
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibitors of human EZH2, and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 8.09 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3984929 | — | — | 1 | 9.10 |
| CHEMBL3701043 | — | — | 1 | 9.10 |
| CHEMBL3957571 | — | — | 1 | 8.89 |
| CHEMBL3896120 | — | — | 1 | 8.82 |
| CHEMBL3908410 | — | — | 1 | 8.82 |
| CHEMBL3938638 | — | — | 1 | 8.80 |
| CHEMBL3956266 | — | — | 1 | 8.80 |
| CHEMBL3701005 | — | — | 1 | 8.72 |
| CHEMBL3910693 | — | — | 1 | 8.66 |
| CHEMBL3955394 | — | — | 1 | 8.66 |
| CHEMBL3770184 | — | — | 1 | 8.66 |
| CHEMBL3909511 | — | — | 1 | 8.64 |
| CHEMBL3701041 | — | — | 1 | 8.57 |
| CHEMBL3916617 | — | — | 1 | 8.57 |
| CHEMBL3701033 | — | — | 1 | 8.55 |
| CHEMBL3971862 | — | — | 1 | 8.55 |
| CHEMBL3940475 | — | — | 1 | 8.54 |
| CHEMBL3961483 | — | — | 1 | 8.54 |
| CHEMBL3701034 | — | — | 1 | 8.51 |
| CHEMBL3911120 | — | — | 1 | 8.47 |
| CHEMBL3909279 | — | — | 1 | 8.46 |
| CHEMBL3701037 | — | — | 1 | 8.46 |
| CHEMBL3909972 | — | — | 1 | 8.42 |
| CHEMBL3904367 | — | — | 1 | 8.40 |
| CHEMBL3942268 | — | — | 1 | 8.40 |
| CHEMBL3939074 | — | — | 1 | 8.38 |
| CHEMBL3933289 | — | — | 1 | 8.35 |
| CHEMBL3701042 | — | — | 1 | 8.34 |
| CHEMBL3918450 | — | — | 1 | 8.32 |
| CHEMBL3932210 | — | — | 1 | 8.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3984929 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3701043 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3957571 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3896120 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3908410 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3938638 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3956266 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3701005 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3910693 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3955394 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3770184 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3909511 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3701041 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3916617 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3971862 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3701033 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3940475 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3961483 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3701034 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3911120 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3909279 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3701037 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3909972 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3904367 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3942268 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3939074 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3933289 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3701042 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3918450 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3932210 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3902888 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3937573 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3963830 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3932366 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3701035 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3893981 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3909934 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3979717 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3916086 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3971620 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3360855 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL3701032 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL3949741 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL3925098 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL3964569 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3941351 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL3946376 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL3942740 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL3945718 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3895049 | — | IC50 | = | 19.2 | nM | 7.72 |