Assay Detail
Binding
CHEMBL4137466
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay
39
Total Activities
39
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
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.49 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170225 | — | — | 1 | 9.30 |
| CHEMBL4162206 | — | — | 1 | 9.15 |
| CHEMBL4160008 | — | — | 1 | 8.70 |
| CHEMBL4159604 | — | — | 1 | 8.70 |
| CHEMBL4173626 | — | — | 1 | 8.52 |
| CHEMBL4171233 | — | — | 1 | 8.52 |
| CHEMBL4163329 | — | — | 1 | 8.22 |
| CHEMBL4163369 | — | — | 1 | 8.22 |
| CHEMBL4173668 | — | — | 1 | 8.22 |
| CHEMBL4173662 | — | — | 1 | 8.15 |
| CHEMBL4170114 | — | — | 1 | 8.10 |
| CHEMBL4177036 | — | — | 1 | 7.92 |
| CHEMBL4175084 | — | — | 1 | 7.82 |
| CHEMBL4174724 | — | — | 1 | 7.82 |
| CHEMBL4167925 | — | — | 1 | 7.77 |
| CHEMBL4162911 | — | — | 1 | 7.66 |
| CHEMBL4176464 | — | — | 1 | 7.62 |
| CHEMBL4166410 | — | — | 1 | 7.57 |
| CHEMBL4164497 | — | — | 1 | 7.40 |
| CHEMBL4162967 | — | — | 1 | 7.38 |
| CHEMBL4159597 | — | — | 1 | 7.37 |
| CHEMBL4161915 | — | — | 1 | 7.36 |
| CHEMBL4159955 | — | — | 1 | 7.32 |
| CHEMBL4175132 | — | — | 1 | 7.28 |
| CHEMBL1231795 | — | — | 1 | 7.26 |
| CHEMBL4171275 | — | — | 1 | 6.87 |
| CHEMBL4162957 | — | — | 1 | 6.85 |
| CHEMBL4167876 | — | — | 1 | 6.83 |
| CHEMBL4164446 | — | — | 1 | 6.58 |
| CHEMBL4170228 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170225 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4162206 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4159604 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4160008 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4173626 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4171233 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4163329 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4163369 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4173668 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4173662 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4170114 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4177036 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4175084 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4174724 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4167925 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4162911 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4176464 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4166410 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4164497 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4162967 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4159597 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4161915 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4159955 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4175132 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1231795 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4171275 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4162957 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4167876 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4164446 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4170228 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL4166822 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL4169833 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL569864 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4166777 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL4174677 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL2336409 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1201129 | DECITABINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL1489 | AZACITIDINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL2441082 | — | IC50 | < | 2.5 | nM | - |