Assay Detail
Binding
CHEMBL4262303
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human G9a using biotinylated peptide H3( 1 to 25 residues) as substrate measured after 15 mins in presence of [3H]-SAM by scintillation proximity assay
77
Total Activities
77
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 | 77 | 6.55 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4287479 | — | — | 1 | 8.40 |
| CHEMBL4290900 | — | — | 1 | 8.10 |
| CHEMBL4294283 | — | — | 1 | 8.00 |
| CHEMBL3621579 | — | — | 1 | 7.89 |
| CHEMBL3621580 | — | — | 1 | 7.68 |
| CHEMBL4286398 | — | — | 1 | 7.60 |
| CHEMBL4287643 | — | — | 1 | 7.52 |
| CHEMBL4291978 | — | — | 1 | 7.41 |
| CHEMBL4284108 | — | — | 1 | 7.41 |
| CHEMBL4285987 | — | — | 1 | 7.31 |
| CHEMBL4278065 | — | — | 1 | 7.26 |
| CHEMBL4282606 | — | — | 1 | 7.26 |
| CHEMBL569864 | — | — | 1 | 7.17 |
| CHEMBL4282018 | — | — | 1 | 7.11 |
| CHEMBL1895209 | — | — | 1 | 7.00 |
| CHEMBL4285447 | — | — | 1 | 6.95 |
| CHEMBL4293686 | — | — | 1 | 6.94 |
| CHEMBL4281773 | — | — | 1 | 6.94 |
| CHEMBL4289892 | — | — | 1 | 6.94 |
| CHEMBL4279738 | — | — | 1 | 6.92 |
| CHEMBL1232432 | — | — | 1 | 6.91 |
| CHEMBL4284947 | — | — | 1 | 6.91 |
| CHEMBL4286468 | — | — | 1 | 6.89 |
| CHEMBL4283093 | — | — | 1 | 6.88 |
| CHEMBL4293277 | — | — | 1 | 6.77 |
| CHEMBL4291748 | — | — | 1 | 6.73 |
| CHEMBL4292456 | — | — | 1 | 6.68 |
| CHEMBL4293645 | — | — | 1 | 6.65 |
| CHEMBL4281116 | — | — | 1 | 6.53 |
| CHEMBL4281519 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4287479 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4290900 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4294283 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3621579 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3621580 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4286398 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4287643 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4291978 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4284108 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4285987 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4278065 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4282606 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL569864 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4282018 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1895209 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4285447 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4293686 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4281773 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4289892 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4279738 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL1232432 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4284947 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4286468 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL4283093 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4293277 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL4291748 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4292456 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4293645 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4281116 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4281519 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4282170 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL4293996 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL1902352 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL4293660 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL4285784 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL4279590 | — | IC50 | = | 575.0 | nM | 6.24 |
| CHEMBL570120 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL4286827 | — | IC50 | = | 683.0 | nM | 6.17 |
| CHEMBL4294768 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4283414 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4290452 | — | IC50 | = | 843.0 | nM | 6.07 |
| CHEMBL4278552 | — | IC50 | = | 869.0 | nM | 6.06 |
| CHEMBL4279942 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4294728 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4295101 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4290591 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4286868 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4291579 | — | IC50 | = | 1018.0 | nM | 5.99 |
| CHEMBL4287174 | — | IC50 | = | 1214.0 | nM | 5.92 |
| CHEMBL4278524 | — | IC50 | = | 1326.0 | nM | 5.88 |