Assay Detail
Binding
CHEMBL3112253
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Inhibition of recombinant JMJD2E (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method
9
Total Activities
9
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
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.55 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230640 | — | — | 1 | 6.52 |
| CHEMBL3108958 | — | — | 1 | 6.38 |
| CHEMBL3108954 | — | — | 1 | 5.46 |
| CHEMBL3108952 | — | — | 1 | 5.41 |
| CHEMBL3108956 | — | — | 1 | 5.30 |
| CHEMBL3108955 | — | — | 1 | 5.29 |
| CHEMBL3108953 | — | — | 1 | 5.26 |
| CHEMBL3108959 | — | — | 1 | 4.80 |
| CHEMBL1255743 | TRANYLCYPROMINE HYDROCHLORIDE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230640 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3108958 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3108954 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3108952 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3108956 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3108955 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3108953 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3108959 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1255743 | TRANYLCYPROMINE HYDROCHLORIDE | IC50 | > | 100000.0 | nM | - |