Assay Detail
Binding
CHEMBL3749873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.10 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3663243 | — | — | 1 | 9.70 |
| CHEMBL3663244 | — | — | 1 | 9.30 |
| CHEMBL3663316 | — | — | 1 | 9.30 |
| CHEMBL3663253 | — | — | 1 | 9.22 |
| CHEMBL3663242 | — | — | 1 | 9.15 |
| CHEMBL3663255 | — | — | 1 | 9.15 |
| CHEMBL3663239 | — | — | 1 | 9.00 |
| CHEMBL3663254 | — | — | 1 | 8.72 |
| CHEMBL3663240 | — | — | 1 | 8.47 |
| CHEMBL3663305 | — | — | 1 | 8.47 |
| CHEMBL3663308 | — | — | 1 | 8.44 |
| CHEMBL3663258 | — | — | 1 | 8.42 |
| CHEMBL3663249 | — | — | 1 | 8.38 |
| CHEMBL3663275 | — | — | 1 | 8.37 |
| CHEMBL3663313 | — | — | 1 | 7.19 |
| CHEMBL3663306 | — | — | 1 | 7.14 |
| CHEMBL3663301 | — | — | 1 | 6.67 |
| CHEMBL3663230 | — | — | 1 | 6.36 |
| CHEMBL3663241 | — | — | 1 | 5.33 |
| CHEMBL3663300 | — | — | 1 | 5.16 |
| CHEMBL3746675 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3663243 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3663244 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3663316 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3663253 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3663242 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3663255 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3663239 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3663254 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3663240 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3663305 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3663308 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3663258 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3663249 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3663275 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3663313 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3663306 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3663301 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL3663230 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3663241 | — | IC50 | = | 4710.0 | nM | 5.33 |
| CHEMBL3663300 | — | IC50 | = | 6960.0 | nM | 5.16 |
| CHEMBL3746675 | — | IC50 | > | 10000.0 | nM | - |