Assay Detail
Binding
CHEMBL4400613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
8-Hydroxy-2-(1H-1,2,3-triazol-1-yl)-1,4-naphtoquinone derivatives inhibited P2X7 Receptor-Induced dye uptake into murine Macrophages.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.40 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445773 | — | — | 1 | 6.99 |
| CHEMBL4454986 | — | — | 1 | 6.64 |
| CHEMBL255787 | — | — | 1 | 6.12 |
| CHEMBL4173394 | BRILLIANT BLUE G | 4.0 | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445773 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4454986 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL255787 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4173394 | BRILLIANT BLUE G | IC50 | = | 1370.0 | nM | 5.86 |