Assay Detail
Binding
CHEMBL3707775
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding Assay: Radioligand binding: human or rat P2X7-1321N1 cells were collected and frozen @ −80° C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 μl:10 μl compound (10×)+(b) 40 μl tracer (2.5×)+50 μl membrane (2×). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2009, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4° C. The assay was terminated by filtration (GF/B filters pre-soaked with 0.3% PEI) and washed with washing buffer (Tris-HCl 50 mM).
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | P2X7-1321N1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
[1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.39 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3663316 | — | — | 1 | 9.40 |
| CHEMBL3663257 | — | — | 1 | 9.40 |
| CHEMBL3663252 | — | — | 1 | 9.00 |
| CHEMBL3663242 | — | — | 1 | 8.96 |
| CHEMBL3663298 | — | — | 1 | 8.80 |
| CHEMBL3663297 | — | — | 1 | 8.74 |
| CHEMBL3663244 | — | — | 1 | 8.70 |
| CHEMBL3663253 | — | — | 1 | 8.70 |
| CHEMBL3663259 | — | — | 1 | 8.55 |
| CHEMBL3663249 | — | — | 1 | 8.49 |
| CHEMBL3663247 | — | — | 1 | 8.46 |
| CHEMBL3663246 | — | — | 1 | 8.30 |
| CHEMBL3663269 | — | — | 1 | 8.30 |
| CHEMBL3663243 | — | — | 1 | 8.30 |
| CHEMBL3663255 | — | — | 1 | 8.30 |
| CHEMBL3663254 | — | — | 1 | 8.25 |
| CHEMBL3663245 | — | — | 1 | 8.20 |
| CHEMBL3663230 | — | — | 1 | 7.90 |
| CHEMBL3663312 | — | — | 1 | 7.79 |
| CHEMBL3663248 | — | — | 1 | 7.60 |
| CHEMBL3663313 | — | — | 1 | 7.50 |
| CHEMBL3663314 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3663316 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3663257 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3663252 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3663242 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3663298 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3663297 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3663244 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3663253 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3663259 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3663249 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3663247 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3663246 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3663269 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3663243 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3663255 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3663254 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL3663245 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3663230 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL3663312 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL3663248 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL3663313 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL3663314 | — | Ki | = | 123.0 | nM | 6.91 |