Assay Detail
Binding
CHEMBL3776389
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDM2A (unknown origin) using biotin-H3K36me2 (28 to 48 residues) as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by alphascreen assay
7
Total Activities
7
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 |
Publication
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.31 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774692 | — | — | 1 | 5.92 |
| CHEMBL3775668 | — | — | 1 | 5.62 |
| CHEMBL3775894 | — | — | 1 | 5.62 |
| CHEMBL3775977 | — | — | 1 | 5.17 |
| CHEMBL3775899 | — | — | 1 | 5.07 |
| CHEMBL3774537 | — | — | 1 | 4.89 |
| CHEMBL3774747 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774692 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3775668 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3775894 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3775977 | — | IC50 | = | 6740.0 | nM | 5.17 |
| CHEMBL3775899 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3774537 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL3774747 | — | IC50 | = | 13400.0 | nM | 4.87 |