Assay Detail
Binding
CHEMBL3772972
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Inhibition of KDM5C catalytic domain (1 -764 aa) (unknown origin) expressed in Sf9 cells using H3K4Me3 peptide as substrate by RFMS assay
6
Total Activities
6
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 |
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 | 6 | 6.55 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3771180 | — | — | 1 | 7.20 |
| CHEMBL3771198 | — | — | 1 | 7.10 |
| CHEMBL3769511 | — | — | 1 | 6.90 |
| CHEMBL3769724 | — | — | 1 | 6.90 |
| CHEMBL3770740 | — | — | 1 | 6.70 |
| CHEMBL3770732 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3771180 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3771198 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3769511 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3769724 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3770740 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3770732 | — | IC50 | = | 31622.78 | nM | 4.50 |