Assay Detail
Binding
CHEMBL3772973
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Inhibition of human KDM5C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.24 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3769724 | — | — | 2 | 5.60 |
| CHEMBL3771198 | — | — | 2 | 5.60 |
| CHEMBL3771180 | — | — | 2 | 5.60 |
| CHEMBL3770740 | — | — | 1 | 4.50 |
| CHEMBL3769511 | — | — | 1 | 4.30 |
| CHEMBL3770732 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3771198 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3769724 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3771198 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3771180 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3771180 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3769724 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3770740 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3769511 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3770732 | — | IC50 | > | 100000.0 | nM | - |