Assay Detail
Binding
CHEMBL4035843
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Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 level after 5 days by mass-spectrometric method
14
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.71 | 6.02 |
| IC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4088737 | — | — | 1 | 6.02 |
| CHEMBL4059597 | — | — | 3 | 5.82 |
| CHEMBL4060968 | — | — | 2 | 5.80 |
| CHEMBL4071387 | — | — | 1 | 5.19 |
| CHEMBL4083572 | — | — | 3 | - |
| CHEMBL4099924 | — | — | 1 | - |
| CHEMBL4081928 | — | — | 1 | - |
| CHEMBL4061676 | — | — | 1 | - |
| CHEMBL4089789 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4088737 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4059597 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4060968 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4071387 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4083572 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4083572 | — | IC50 | - | — | - | |
| CHEMBL4083572 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4099924 | — | EC50 | - | — | - | |
| CHEMBL4081928 | — | EC50 | - | — | - | |
| CHEMBL4061676 | — | EC50 | - | — | - | |
| CHEMBL4089789 | — | EC50 | - | — | - | |
| CHEMBL4059597 | — | EC50 | - | — | - | |
| CHEMBL4059597 | — | EC50 | - | — | - | |
| CHEMBL4060968 | — | EC50 | - | — | - |