Assay Detail
Binding
CHEMBL5682504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6/Flag-tagged TEV-protease cleavage site fused JMJD3 1637-1675 deletion mutant (1141 to 1682 residues) expressed in baculovirus infected Sf9 insect cells using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry
4
Total Activities
4
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
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.30 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3188597 | — | — | 1 | 5.30 |
| CHEMBL4303308 | — | — | 1 | - |
| CHEMBL3183531 | — | — | 1 | - |
| CHEMBL4786329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3188597 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4303308 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3183531 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4786329 | — | IC50 | > | 50000.0 | nM | - |