Assay Detail
Binding
CHEMBL4353692
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Inhibition of KDM2A (unknown origin) by Alphascreen assay
6
Total Activities
6
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
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.43 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4585876 | — | — | 1 | 5.85 |
| CHEMBL4592908 | — | — | 1 | 5.71 |
| CHEMBL4516101 | — | — | 1 | 5.42 |
| CHEMBL4449500 | — | — | 1 | 5.35 |
| CHEMBL4447515 | — | — | 1 | 5.33 |
| CHEMBL4525269 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4585876 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4592908 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4516101 | — | IC50 | = | 3770.0 | nM | 5.42 |
| CHEMBL4449500 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4447515 | — | IC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL4525269 | — | IC50 | = | 12540.0 | nM | 4.90 |