Assay Detail
Binding
CHEMBL4056672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human G9a catalytic domain (913 to 1193 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated H3 (1 to 25 residues) as substrate preincubated for 20 mins in presence of [3H]SAM measured after 2 hrs by scintillation proximity assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EHMT2 (CHEMBL6032) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.38 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066769 | — | — | 1 | 7.04 |
| CHEMBL4088064 | — | — | 1 | 6.96 |
| CHEMBL4075387 | — | — | 1 | 6.82 |
| CHEMBL4100004 | — | — | 1 | 6.75 |
| CHEMBL576260 | — | — | 1 | 6.72 |
| CHEMBL4094717 | — | — | 1 | 6.59 |
| CHEMBL4069640 | — | — | 1 | 6.55 |
| CHEMBL4072211 | — | — | 1 | 6.53 |
| CHEMBL4084508 | — | — | 1 | 6.50 |
| CHEMBL4104425 | — | — | 1 | 6.50 |
| CHEMBL585180 | — | — | 1 | 6.46 |
| CHEMBL4074209 | — | — | 1 | 6.45 |
| CHEMBL4064559 | — | — | 1 | 6.45 |
| CHEMBL4101782 | — | — | 1 | 6.35 |
| CHEMBL4092975 | — | — | 1 | 6.33 |
| CHEMBL4063767 | — | — | 1 | 6.32 |
| CHEMBL4072358 | — | — | 1 | 6.32 |
| CHEMBL4105129 | — | — | 1 | 6.29 |
| CHEMBL4090654 | — | — | 1 | 6.27 |
| CHEMBL4068291 | — | — | 1 | 6.27 |
| CHEMBL4102467 | — | — | 1 | 6.26 |
| CHEMBL4093972 | — | — | 1 | 6.23 |
| CHEMBL4095652 | — | — | 1 | 6.14 |
| CHEMBL4092251 | — | — | 1 | 6.14 |
| CHEMBL4080189 | — | — | 1 | 6.10 |
| CHEMBL4083783 | — | — | 1 | 6.02 |
| CHEMBL4073147 | — | — | 1 | 5.94 |
| CHEMBL4076634 | — | — | 1 | 5.80 |
| CHEMBL4082847 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066769 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4088064 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4075387 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4100004 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL576260 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4094717 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL4069640 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL4072211 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4084508 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4104425 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL585180 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4074209 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4064559 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL4101782 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL4092975 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL4063767 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL4072358 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL4105129 | — | IC50 | = | 508.0 | nM | 6.29 |
| CHEMBL4090654 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL4068291 | — | IC50 | = | 532.0 | nM | 6.27 |
| CHEMBL4102467 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4093972 | — | IC50 | = | 585.0 | nM | 6.23 |
| CHEMBL4095652 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL4092251 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL4080189 | — | IC50 | = | 788.0 | nM | 6.10 |
| CHEMBL4083783 | — | IC50 | = | 956.0 | nM | 6.02 |
| CHEMBL4073147 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4076634 | — | IC50 | = | 1582.0 | nM | 5.80 |
| CHEMBL4082847 | — | IC50 | = | 1630.0 | nM | 5.79 |