Assay Detail
Binding
CHEMBL4262314
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of G9a (913 to 1193 residues) (unknown origin) using peptide H3 (1 to 25 residues) as substrate pretreated for 5 mins followed by substrate addition by Thioglo reagent based enzyme coupled SAH detection assay
11
Total Activities
11
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
Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.43 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576781 | — | — | 1 | 7.37 |
| CHEMBL1213766 | — | — | 1 | 6.96 |
| CHEMBL569864 | — | — | 1 | 6.96 |
| CHEMBL578227 | — | — | 1 | 6.48 |
| CHEMBL572373 | — | — | 1 | 6.17 |
| CHEMBL585180 | — | — | 1 | 6.04 |
| CHEMBL576260 | — | — | 1 | 5.96 |
| CHEMBL1213959 | — | — | 1 | 5.47 |
| CHEMBL1213957 | — | — | 1 | - |
| CHEMBL1213903 | — | — | 1 | - |
| CHEMBL1213960 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576781 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1213766 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL569864 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL578227 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL572373 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL585180 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL576260 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1213959 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1213957 | — | IC50 | = | 25.0 | nM | - |
| CHEMBL1213903 | — | IC50 | = | 8.0 | nM | - |
| CHEMBL1213960 | — | IC50 | > | 10000.0 | nM | - |