Assay Detail
Binding
CHEMBL3789200
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Inhibition of recombinant full length FLAG-tagged KDM5A (unknown origin) expressed in sf9 cells using biotin-H3K4me3 (1 to 21 residues as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by mass spetcrometric analysis
5
Total Activities
5
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
Recent Progress in Histone Demethylase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.58 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786038 | — | — | 1 | 8.64 |
| CHEMBL3785583 | — | — | 1 | 7.85 |
| CHEMBL3785443 | — | — | 1 | 7.82 |
| CHEMBL3786862 | — | — | 1 | 6.00 |
| CHEMBL3786528 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786038 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3785583 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3785443 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3786862 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3786528 | — | IC50 | < | 1000.0 | nM | - |