Assay Detail
Binding
CHEMBL4223293
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Inhibition of KDM5A/KDM5B in human ZR-75-1 cells assessed as increase in H3K4me3 level after 72 hrs by fluorometric immunoassay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | ZR-75-1 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Target
Lysine-specific demethylase 5A/5B (CHEMBL4296073) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Structure-based design and discovery of potent and selective KDM5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.99 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786952 | — | — | 1 | 7.05 |
| CHEMBL4228292 | — | — | 1 | 6.96 |
| CHEMBL3785832 | — | — | 1 | 6.38 |
| CHEMBL4227526 | — | — | 1 | 6.10 |
| CHEMBL4225013 | — | — | 1 | 6.08 |
| CHEMBL4226978 | — | — | 1 | 6.07 |
| CHEMBL4229271 | — | — | 1 | 6.03 |
| CHEMBL4228087 | — | — | 1 | 6.00 |
| CHEMBL4229264 | — | — | 1 | 6.00 |
| CHEMBL4227237 | — | — | 1 | 5.89 |
| CHEMBL4228546 | — | — | 1 | 5.89 |
| CHEMBL4228806 | — | — | 1 | 5.34 |
| CHEMBL4225358 | — | — | 1 | 5.16 |
| CHEMBL4228781 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786952 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4228292 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3785832 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4227526 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4225013 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4226978 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4229271 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4228087 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4229264 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4227237 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4228546 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4228806 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4225358 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4228781 | — | EC50 | = | 12000.0 | nM | 4.92 |