Assay Detail
Binding
CHEMBL4270047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDM6A (880 to 1401 residues) (unknown origin) using H3 ( 21 to 44 residues) K27me3 as substrate preincubated for 15 min followed by substrate addition measured after 15 mins by FDH-coupled demethylase assay
3
Total Activities
3
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
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.28 | 4.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4283844 | — | — | 1 | 4.41 |
| CHEMBL4294426 | — | — | 1 | 4.26 |
| CHEMBL3188597 | — | — | 1 | 4.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4283844 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4294426 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL3188597 | — | IC50 | = | 69000.0 | nM | 4.16 |