Assay Detail
Binding
CHEMBL4350283
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Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EHMT1 (CHEMBL6031) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 6.50 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4582775 | — | — | 1 | 8.22 |
| CHEMBL4461224 | — | — | 1 | 8.05 |
| CHEMBL4467219 | — | — | 1 | 8.05 |
| CHEMBL3109630 | — | — | 1 | 7.96 |
| CHEMBL4568910 | — | — | 1 | 7.96 |
| CHEMBL4464846 | — | — | 1 | 7.92 |
| CHEMBL4532743 | — | — | 1 | 7.92 |
| CHEMBL1231795 | — | — | 1 | 7.89 |
| CHEMBL4460703 | — | — | 1 | 7.80 |
| CHEMBL4560792 | — | — | 1 | 7.72 |
| CHEMBL4452780 | — | — | 1 | 7.72 |
| CHEMBL4435107 | — | — | 1 | 7.72 |
| CHEMBL576781 | — | — | 1 | 7.64 |
| CHEMBL4552592 | — | — | 1 | 7.57 |
| CHEMBL4555461 | — | — | 1 | 7.46 |
| CHEMBL4438513 | — | — | 1 | 7.39 |
| CHEMBL4460246 | — | — | 1 | 7.36 |
| CHEMBL4474688 | — | — | 1 | 7.33 |
| CHEMBL4476055 | — | — | 1 | 7.16 |
| CHEMBL4475124 | — | — | 1 | 7.11 |
| CHEMBL4564339 | — | — | 1 | 7.03 |
| CHEMBL4558425 | — | — | 1 | 6.91 |
| CHEMBL4580258 | — | — | 1 | 6.82 |
| CHEMBL4570643 | — | — | 1 | 6.82 |
| CHEMBL4445273 | — | — | 1 | 6.75 |
| CHEMBL4483418 | — | — | 1 | 6.69 |
| CHEMBL4454215 | — | — | 1 | 6.55 |
| CHEMBL4449387 | — | — | 1 | 6.52 |
| CHEMBL4531347 | — | — | 1 | 6.28 |
| CHEMBL4576128 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4582775 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4461224 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4467219 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3109630 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4568910 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4464846 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4532743 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1231795 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4460703 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4560792 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4452780 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4435107 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL576781 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4552592 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4555461 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4438513 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4460246 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4474688 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4476055 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4475124 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4564339 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4558425 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4580258 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4570643 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4445273 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4483418 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4454215 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4449387 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4531347 | — | IC50 | = | 529.0 | nM | 6.28 |
| CHEMBL4576128 | — | IC50 | = | 647.0 | nM | 6.19 |
| CHEMBL4521601 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL4472965 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL4459846 | — | IC50 | = | 698.0 | nM | 6.16 |
| CHEMBL4539095 | — | IC50 | = | 885.0 | nM | 6.05 |
| CHEMBL4455940 | — | IC50 | = | 926.0 | nM | 6.03 |
| CHEMBL4474589 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL4450948 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4566722 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4549942 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4470252 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4443408 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL4525421 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4483651 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4554966 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL4565082 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL4542297 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4576112 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL4529430 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL4532481 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL4467642 | — | IC50 | = | 2860.0 | nM | 5.54 |